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Sample records for anti-infective activity screening

  1. 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.

  2. 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.

  3. 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.

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

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

    2015-07-01

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2016-01-01

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2016-01-01

    Objective: To search for the most active antimicrobial and antioxidant sub-fractions related to traditional use of Ziziphus oxyphylla(Z. oxyphylla) and Cedrela serrata(C. serrata) in Pakistan against infectious and liver diseases.Methods: Factions of different polarity were tested in vitro for their antiprotozoal,antimalarial, antibacterial and antifungal activity against different pathogens. Cytotoxicity on MRC-5 cell lines(human lung fibroblasts) as well as, in vitro radical scavenging activity was evaluated using the 1, 1-diphenyl-2-picrylhydrazyl radical assay.Results: The highest antiprotozoal activity was observed for the CHCl3 fractions of Z. oxyphylla roots and leaves, and C. serrata bark. The CHCl3 and Et OAc fractions of Z. oxyphylla roots, the CHCl3 fraction of Z. oxyphylla leaves, the Et OAc and the residual Me OH: H2 O fraction of C. serrata bark showed antibacterial activity against Staphylococcus aureus. The same residual Me OH: H2 O fraction of C. serrata bark was active against Candida albicans. The highest antioxidant activity was observed for the more hydrophilic Et OAc fractions of Z. oxyphylla leaves, C. serrata bark and leaves, and the residual Me OH: H2 O fraction of C. serrata bark.Conclusions: This study supports at least in part the traditional uses of these plants for antimicrobial purposes and against liver diseases.

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

    Directory of Open Access Journals (Sweden)

    Cristiana da Purificação Pinto

    2013-01-01

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

  8. Anti-infective potential of hot-spring bacteria

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    Pallavi Pednekar

    2011-01-01

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

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

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    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.

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

    Science.gov (United States)

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

    2011-05-01

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

  11. 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.

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

    DEFF Research Database (Denmark)

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

    2010-01-01

    Virulent factors produced by pathogens play an important role in the infectious process, which is regulated by a cell-to-cell communication mechanism called quorum sensing (QS). Pseudomonas aeruginosa is an important opportunistic human pathogen, which causes infections in patients with compromised...... of ginseng are mutually exclusive as it is a complex mixture, as shown with the HPLC analysis of the hot water extract. Though ginseng is a promising natural synergetic remedy, it is important to isolate and evaluate the ginseng compounds associated with the anti-QS activity....

  13. [Anti-infective phytotherapies of the tree-savannah, Senegal (occidental Africa). III: A review of phytochemical substances and the antimicrobial activity of 43 species].

    Science.gov (United States)

    Le Grand, A

    1989-05-01

    A review has been made of the ethnobotanical and pharmacological data of 43 medicinal plants of the tree-savannah used by the Diola against infectious diseases. The traditional use of ten plants can be explained by pharmacologically active principles: Adansonia digitata, Azadirachta indica, Carica papaya, Cassia tora, Fagara leprieurii, Guiera senegalensis, Khaya senegalensis, Mangifera indica, Psidium guajava and Voacanga africana. Four of these herbs are recommended for use in Primary Health Care. The therapeutic value of the other plants discussed is not absolutely clear. It is, however, obvious that herbal medicine has a large potential, which is still insufficiently explored, for utilization in Primary Health Care.

  14. Avian cathelicidins: paradigms for the development of anti-infectives.

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    van Dijk, A; Molhoek, E M; Bikker, F J; Yu, P-L; Veldhuizen, E J A; Haagsman, H P

    2011-11-21

    The broad-spectrum defense system based on host defense peptides (HDPs) is evolutionary very old and many invertebrates rely on this system for protection from bacterial infections. However, in vertebrates the system remained important in spite of the superposition of a very sophisticated adaptive immune system. The cathelicidins comprise a major group of HDPs in mammals. About six years ago it was first described that cathelicidins are also present in birds. Here we review the properties and biological activities of the recently discovered avian cathelicidins and their potential to be used as a paradigm for the development of anti-infectives. Like the mammalian cathelicidins, avian cathelicidins exert direct antimicrobial activities but can also selectively boost host immune responses by regulation of cytokine production and recruitment of immune cells. In addition, it was found that chicken cathelicidins bind endotoxins and dampen the endotoxin-mediated inflammatory response. Molecular dissection has allowed identification of different structural elements involved in bacterial killing and immunomodulation. These studies have enabled the design of small HDP-based antibiotics with specific functions, i.e. having primarily immunomodulatory or antimicrobial activities. Since the immunomodulatory effects may, to a certain degree, be species-specific, we hypothesize that poultry-specific antibiotics can be developed based on avian cathelicidins.

  15. Anti-infective potential of Citrus bergamia Risso et Poiteau (bergamot) derivatives: a systematic review.

    Science.gov (United States)

    Cirmi, Santa; Bisignano, Carlo; Mandalari, Giuseppina; Navarra, Michele

    2016-09-01

    Infectious diseases remain among the leading causes of morbidity and mortality worldwide, mainly because of the increase of resistance to chemotherapeutic drugs. Nature is the major source of anti-infective drugs and could represent a font of medicines that may help overcome antibiotic resistance. Recently, the potential antimicrobial effect of certain plant extracts has attracted attention within the scientific community as alternatives to synthetic drugs. Here, we present a systematic review on the anti-infective properties of bergamot derivatives that highlight the activity of bergamot essential oil against bacteria, mycetes and larvae, as well as the anti-Helicobacter pylori effect of bergamot juice and the antimicrobial properties of extracts from bergamot peel. Findings presented herein could be used to develop novel and alternative preventive and therapeutic strategies aimed to overcome antibiotic resistance. Copyright © 2016 John Wiley & Sons, Ltd.

  16. 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.

  17. NEW ASPECTS OF ANTI-INFECTION IMMUNITY

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    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.

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

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

    2014-09-01

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

  19. Screening Of Marine Bacteria For Pharmacological Activities

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    S. Vijayalakshmi

    2015-08-01

    Full Text Available Abstract The symbiotic and associated four marine bacteria BR1 Flavobacterium sp. isolated from Barnacle Balanus amphitriteEM13 Micrococus sp. from Seaweed Enteromorpha compressaPC4 Alcaligenes sp. from Ascidian Polyclinum constellatum and SW12 Bacillus sp. from seawater were cultured and extracted for pharmacological activities. The ethyl acetate extracts of these marine bacterial culture supernatants were screened for pharmacological activities such as Anti inflammatory Analgesic and CNS depressant activities using experimental animal model. In this studySW12 exhibited high activity for both Anti inflammatory and Analgesic. Especially which exhibited highest analgesic activity than standard drug pethidine. Another one PC4 showed highest analgesic activity similar to standard drug. Other two extracts EM13 and BR1 showed high activity in CNS depressant. Based on the result SW12 is a highly potent strain it may produce novel compound for pharmacological drug.

  20. Study of the Active Screen Plasma Nitriding

    Institute of Scientific and Technical Information of China (English)

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

    2004-01-01

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

  1. Emerging paradigms in anti-infective drug design.

    Science.gov (United States)

    Barrett, Michael P; Croft, Simon L

    2014-01-01

    The need for new drugs to treat microbial infections is pressing. The great progress made in the middle part of the twentieth Century was followed by a period of relative inactivity as the medical needs relating to infectious disease in the wealthier nations receded. Growing realisation that anti-infectives are needed in many parts of the world, to treat neglected diseases as well as to combat the burgeoning risk of resistance to existing drugs, has galvanised a new wave of research into anti-microbial drugs. The transfer of knowledge from the Pharmaceutical industry relating to the importance of understanding how to target drugs successfully within the body, and improved understanding of how pathogens interact with their hosts, is driving a series of new paradigms in anti-infective drug design. Here we provide an overview of those processes as an introduction to a series of articles from experts in this area that emerged from a meeting entitled "Emerging Paradigms in Anti-Infective Drug Design" held in London on the 17th and 18th September 2012. The symposium was organised jointly by British Society for Parasitology (BSP) and the Biological & Medicinal Chemistry sector of the Royal Society of Chemistry (RSC) and held at the London School of Hygiene & Tropical Medicine. The symposium set out to cover all aspects of the identification of new therapeutic modalities for the treatment of neglected and tropical diseases. We aimed to bring together leading scientists from all the disciplines working in this field and cover the pharmacology, medicinal chemistry and drug delivery of potential new medicines. Sessions were held on: "Target diseases and targets for drugs", "Target based medicinal chemistry", "Bioavailability and chemistry", "Targeting intracellular microbes", "Alternative approaches and models", and "New anti-infectives - how do we get there?" This symposium was organised by Simon Croft (LSHTM) and Mike Barrett (University of Glasgow) for the BSP, and David

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

    Science.gov (United States)

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

    2015-01-21

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

  3. PRENYLATED BENZOIC ACID DERIVATIVES FROM PIPER SPECIES AS SOURCE OF ANTI-INFECTIVE AGENTS

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    Ibrahim Malami

    2012-06-01

    Full Text Available A number of prenylated benzoic acids derivatives with interesting biological activities have been previously isolated and characterized from different species of piperaceae family. Several Piper species contained structurally similar compounds with diverse biological activities such as anti-bacterial, anti-fungal, insecticidal as well as anti-parasitic all of which produces compounds that can be classified as prenylated benzoic acid derivatives. Piper sp has proven to serve as a source of potential anti-infective agents by developing a biosynthetic route to the synthesis of prenylated benzoic acids derivative natural products as their chemical defense system. Despite the frequent isolation of these interesting compounds with strong biological activity, yet none have been taking into consideration for development into therapeutic agents.

  4. Anti-infective properties of bacteriocins: an update.

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    Hammami, Riadh; Fernandez, Benoit; Lacroix, Christophe; Fliss, Ismail

    2013-08-01

    Bacteriocin production is a widespread phenomenon among bacteria. Bacteriocins hold great promise for the treatment of diseases caused by pathogenic bacteria and could be used in the future as alternatives to existing antibiotics. The anti-infective potential of bacteriocins for inhibiting pathogens has been shown in various food matrices including cheese, meat, and vegetables. However, their inhibition of pathogens in vivo remains unclear and needs more investigation, due mainly to difficulties associated with demonstrating their health benefits. Many bacteriocins produced by established or potential probiotic organisms have been evaluated as potential therapeutic agents and interesting findings have been documented in vitro as well as in a few in vivo studies. Some recent in vivo studies point to the efficacy of bacteriocin-based treatments of human and animal infections. While further investigation remains necessary before the possibilities for bacteriocins in clinical practice can be described more fully, this review provides an overview of their potential applications to human and veterinary health.

  5. New Anti-Infective Coatings of Medical Implants▿

    Science.gov (United States)

    Matl, F. D.; Obermeier, A.; Repmann, S.; Friess, W.; Stemberger, A.; Kuehn, K.-D.

    2008-01-01

    Implantable devices are highly susceptible to infection and are therefore a major risk in surgery. The present work presents a novel strategy to prevent the formation of a biofilm on polytetrafluoroethylene (PTFE) grafts. PTFE grafts were coated with gentamicin and teicoplanin incorporated into different lipid-like carriers under aseptic conditions in a dipping process. Poly-d,l-lactic acid, tocopherol acetate, the diglyceride Softisan 649, and the triglyceride Dynasan 118 were used as drug carriers. The drug release kinetics, anti-infective characteristics, biocompatibility, and hemocompatibility of the coatings developed were studied. All coatings showed an initial drug burst, followed by a low continuous drug release over 96 h. The dimension of release kinetics depended on the carrier used. All coated prostheses reduced bacterial growth drastically over 24 h, even below pathologically relevant concentrations. Different cytotoxic levels could be observed, revealing tocopherol acetate as the most promising biocompatible carrier. A possible reason for the highly cytotoxic effect of Softisan 649 could be assessed by demonstrating incorporated lipids in the cell soma with Oil Red O staining. Tromboelastography studies, enzyme-linked immunosorbent assays, and an amidolytic substrate assay could confirm the hemocompatibility of individual coatings. The development of the biodegradable drug delivery systems described here and in vitro studies of those systems highlight the most important requirements for effective as well as compatible anti-infective coatings of PTFE grafts. Through continuous local release, high drug levels can be produced at only the targeted area and physiological bacterial proliferation can be completely inhibited, while biocompatibility as well as hemocompatibility can be ensured. PMID:18362194

  6. New anti-infective coatings of medical implants.

    Science.gov (United States)

    Matl, F D; Obermeier, A; Repmann, S; Friess, W; Stemberger, A; Kuehn, K-D

    2008-06-01

    Implantable devices are highly susceptible to infection and are therefore a major risk in surgery. The present work presents a novel strategy to prevent the formation of a biofilm on polytetrafluoroethylene (PTFE) grafts. PTFE grafts were coated with gentamicin and teicoplanin incorporated into different lipid-like carriers under aseptic conditions in a dipping process. Poly-d,l-lactic acid, tocopherol acetate, the diglyceride Softisan 649, and the triglyceride Dynasan 118 were used as drug carriers. The drug release kinetics, anti-infective characteristics, biocompatibility, and hemocompatibility of the coatings developed were studied. All coatings showed an initial drug burst, followed by a low continuous drug release over 96 h. The dimension of release kinetics depended on the carrier used. All coated prostheses reduced bacterial growth drastically over 24 h, even below pathologically relevant concentrations. Different cytotoxic levels could be observed, revealing tocopherol acetate as the most promising biocompatible carrier. A possible reason for the highly cytotoxic effect of Softisan 649 could be assessed by demonstrating incorporated lipids in the cell soma with Oil Red O staining. Tromboelastography studies, enzyme-linked immunosorbent assays, and an amidolytic substrate assay could confirm the hemocompatibility of individual coatings. The development of the biodegradable drug delivery systems described here and in vitro studies of those systems highlight the most important requirements for effective as well as compatible anti-infective coatings of PTFE grafts. Through continuous local release, high drug levels can be produced at only the targeted area and physiological bacterial proliferation can be completely inhibited, while biocompatibility as well as hemocompatibility can be ensured.

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

    Science.gov (United States)

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

    2016-01-01

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

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

    Science.gov (United States)

    Kruse, Thomas; Kristensen, Hans-Henrik

    2008-12-01

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

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

    DEFF Research Database (Denmark)

    Olafsdottir, Steingerdur; Ahrens, Wolfgang; Siani, Alfonso

    2014-01-01

    Background/Objectives: This longitudinal study describes the relationship between young children’s screen time, dietary habits and anthropometric measures. The hypothesis was that television viewing and other screen activities at baseline result in increased consumption of sugar-sweetened beverages...... (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. Subjects/Methods: The study is a part of the prospective cohort study...... 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. Conclusions: The results indicate substantial effects of TV viewing and other screen activities for young...

  10. High Resolution Screening of biologically active compounds and metabolites

    NARCIS (Netherlands)

    Kool, J.

    2007-01-01

    High Resolution Screening of biologically active compounds and metabolites Jeroen Kool Biotransformation enzymes play a crucial role in the metabolism of both endogenous compounds and xenobiotics. Usually, the detoxication of these compounds by biotransformation enzymes results in harmless metab

  11. Screening metagenomic libraries for laccase activities.

    Science.gov (United States)

    Ferrer, Manuel; Beloqui, Ana; Golyshin, Peter N

    2010-01-01

    Laccases are multi-copper oxidoreductases (benzenediol:oxygen oxidoreductases, EC 1.10.3.2) able to oxidise a wide variety of phenolic and non-phenolic compounds. They are useful enzymes for a variety of applications, including bioremediation and craft pulp bio-bleaching as the most significant ones. There is a considerable interest to find new laccases through the exploration of biological diversity. Laccases have been found in plants, insects, and bacteria but predominantly in fungi: these enzymes have been documented in about 60 fungal strains. Microbial diversity constitutes a largely unexplored treasure chest with new laccases with a good potential for basic science and biotechnology. At present, due to our inability to cultivate most microbes, the only means of accessing the resources of the microbial world is to harvest genetic resources ("metagenomes"), which can further on be subjected to extensive screening programs. In this chapter, we provide an overview of screening methods to identify laccase-encoding genes from environmental resources.

  12. 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.

  13. Steroid-decorated antibiotic microparticles for inhaled anti-infective therapy.

    Science.gov (United States)

    Lee, Sie Huey; Teo, Jeanette; Heng, Desmond; Zhao, Yanli; Ng, Wai Kiong; Chan, Hak-Kim; Tan, Reginald B H

    2014-04-01

    Despite advances in vaccination and antimicrobial therapy, community-acquired pneumonia (CAP) remains as a leading cause of morbidity and mortality worldwide. As the severity of CAP has been linked to the extent of inflammation in the body, adjunctive therapeutic measures aimed at modulating the immune response have therefore become increasingly attractive in recent years. In particular, for CAP patients with underlying medical conditions such as chronic obstructive pulmonary disease (COPD), a steroid-antibiotic combination will no doubt be a useful and timely therapeutic intervention. Unfortunately, no combined steroid-antibiotic dry powder formulation is available commercially or has been reported in the academic literature. The aim of this work was hence to develop a novel steroid-antibiotic dry powder inhaler formulation [ciprofloxacin hydrochloride (CIP) and beclomethasone dipropionate (BP)] for inhaled anti-infective therapy. The spray-dried powder was of respirable size (d50 of ∼2.3 μm), partially crystalline and had BP preferentially deposited on the particle surface. Favorably, when formulated as a binary mix, both CIP and BP showed much higher drug release and fine particle fractions (of the loaded dose) over their singly delivered counterparts, and had robust activity against the respiratory tract infection-causing bacteria Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus.

  14. Perspective: On the active site model in computational catalyst screening

    Science.gov (United States)

    Reuter, Karsten; Plaisance, Craig P.; Oberhofer, Harald; Andersen, Mie

    2017-01-01

    First-principles screening approaches exploiting energy trends in surface adsorption represent an unparalleled success story in recent computational catalysis research. Here we argue that our still limited understanding of the structure of active sites is one of the major bottlenecks towards an ever extended and reliable use of such computational screening for catalyst discovery. For low-index transition metal surfaces, the prevalently chosen high-symmetry (terrace and step) sites offered by the nominal bulk-truncated crystal lattice might be justified. For more complex surfaces and composite catalyst materials, computational screening studies will need to actively embrace a considerable uncertainty with respect to what truly are the active sites. By systematically exploring the space of possible active site motifs, such studies might eventually contribute towards a targeted design of optimized sites in future catalysts.

  15. Substrate Activity Screening (SAS) and Related Approaches in Medicinal Chemistry.

    Science.gov (United States)

    Gladysz, Rafaela; Lambeir, Anne-Marie; Joossens, Jurgen; Augustyns, Koen; Van der Veken, Pieter

    2016-03-04

    Substrate activity screening (SAS) was presented a decade ago by Ellman and co-workers as a straightforward methodology for the identification of fragment-sized building blocks for enzyme inhibitors. Ever since, SAS and variations derived from it have been successfully applied to the discovery of inhibitors of various families of enzymatically active drug targets. This review covers key achievements and challenges of SAS and related methodologies, including the modified substrate activity screening (MSAS) approach. Special attention is given to the kinetic and thermodynamic aspects of these methodologies, as a thorough understanding thereof is crucial for successfully transforming the identified fragment-sized hits into potent inhibitors.

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

    Science.gov (United States)

    Conrad, Andreas; Frank, Uwe

    2008-05-01

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

  17. Revealing indigenous Indonesian traditional medicine: anti-infective agents.

    Science.gov (United States)

    Nugraha, Ari S; Keller, Paul A

    2011-12-01

    Indonesia is rich in medicinal plants which the population has used traditionally from generation to generation for curing diseases. Our interest in the treatment of infectious diseases has lead to the investigation of traditional Indonesian treatments. In this review, we present a comprehensive review of ethnopharmacologically directed screening in Indonesian medicinal plants to search for new anti-viral, antimalarial, anti-bacterial and anti-fungal agents. Some potent drug leads have been isolated from Indonesian medicinal plants. Further research is still required for the lead development as well as the search for new bioactive compounds from the enormous medicinal plant resources.

  18. Antimicrobial activity and phytochemical screening 4 of Arbutus unedo L

    OpenAIRE

    Dib, Mohamed El Amine; Allali, Hocine; Bendiabdellah, Amel; Meliani, Nawel; Tabti, Boufeldja

    2012-01-01

    In this study, antimicrobial activities of water and methanol extract, and three phenolic fractions of the roots of Arbutus unedo L. were investigated. Poor antibacterial activity against both Staphylococcus aureus and Pseudomonas aeruginosa bacteria was shown with water and methanol extract. However moderate antibacterial activity was shown by water extract and phenolic fractions against Escherichia coli and S. aureus, respectively. The phytochemical screening of roots of A. u...

  19. 78 FR 48690 - Anti-Infective Drugs Advisory Committee; Notice of Meeting

    Science.gov (United States)

    2013-08-09

    ... the public. Name of Committee: Anti-Infective Drugs Advisory Committee. General Function of the... (involving internal organs), mucosal (involving areas such as inside the mouth and nose), and cutaneous... limited. If the number of registrants requesting to speak is greater than can be reasonably...

  20. 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

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

    Science.gov (United States)

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

    2013-04-24

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

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

    DEFF Research Database (Denmark)

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

    1999-01-01

    Twenty pesticides were tested for their ability to activate the oestrogen receptor in vitro using an,MCF7 cell proliferation assay and a Yeast Oestrogen Screen. The fungicides fenarimol, triadimefon, and triadimenol were identified as weak oestrogen receptor agonists, which at 10 mu M induces a 2...... published that support oestrogenic activity in the intact animal, Thus, from the present results Mie suggest that oestrogen receptor activation may not be an important mode of action for these compounds. The need to include at least two bioassays in a screening procedure and for combining in vitro.......0, 2.4, and 1.9-fold increase in proliferation of human MCF7 breast cancer cells (E3 clone). The relative proliferation efficiency (RPE) was 43-69%, indicating partial agonism at the oestrogen receptor. Several pesticides did not have any effect oil the proliferation response after 6 days of exposure...

  3. 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.

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

    Science.gov (United States)

    Jampilek, Josef

    2014-01-01

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

  5. Novel anti-infective potential of salvianolic acid B against human serious pathogen Neisseria meningitidis

    OpenAIRE

    Huttunen, Sanna; Toivanen, Marko; Liu, Chenghai; Tikkanen-Kaukanen, Carina

    2016-01-01

    Background Epidemics of meningococcal meningitis cause significant health problems especially in Sub-Saharan Africa. Novel anti-infective candidates are needed. In modern anti-adhesion therapy initial attachment of bacteria to host cells is prevented. Our unique studies have revealed anti-adhesive candidates from natural products, namely milk and berries, against Neisseria meningitidis adhesion. In the present study against N. meningitidis adhesion, a novel binding inhibitor was found; salvia...

  6. 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.

  7. Screening of Iranian plants for antifungal activity: Part 2

    Directory of Open Access Journals (Sweden)

    "Amin Gh.R

    2002-08-01

    Full Text Available In this study, 278 species from 37 families of native Iranian plants were screened for in vitro antifungal activity against 19 fungal strains. Initially, the crude extracts in concentration of 100 μg/ml were tested. Among 278 plant extracts, 201(71.27% of them showed antifungal activity against at least one fungal strain. A wide range of total extracts of different species were shown to have potentially noticeable antifungal effects. The outstanding species were: Mentha longifolia, Saliva multicaulis, Thymus transcaspicus, Zataria multiflora, Glycyrrhiza glabra, Hulthemia persica, Heracleum persicum, Pimpinella anisum, Pragnos ferulacea, Pragnos uloptera, and Viola odorata.

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

    Science.gov (United States)

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

    2015-09-01

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

  9. 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 (P<0.05) analgesic 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.

  10. Phytochemical Screening and Antidiarrhoeal Activity of Hyptis suaveolens

    Directory of Open Access Journals (Sweden)

    Md. Zeshan Hashib Shaikat

    2012-08-01

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

  11. 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.

  12. 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.

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

    Science.gov (United States)

    Soufan, Othman; Ba-alawi, Wail; Afeef, Moataz; Essack, Magbubah; Rodionov, Valentin; Kalnis, Panos; Bajic, Vladimir B

    2015-01-01

    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.

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

    Institute of Scientific and Technical Information of China (English)

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

    2016-01-01

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2012-01-01

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

  16. Screening of Crude Plant Extracts with Anti-Obesity Activity

    Directory of Open Access Journals (Sweden)

    Changhyun Roh

    2012-02-01

    Full Text Available Obesity is a global health problem. It is also known to be a risk factor for the development of metabolic disorders, type 2 diabetes, systemic hypertension, cardiovascular disease, dyslipidemia, and atherosclerosis. In this study, we screened crude extracts from 400 plants to test their anti-obesity activity using porcine pancreatic lipase assay (PPL; triacylglycerol lipase, EC 3.1.1.3 in vitro activity. Among the 400 plants species examined, 44 extracts from plants, showed high anti-lipase activity using 2,4-dinitrophenylbutyrate as a substrate in porcine pancreatic lipase assay. Furthermore, 44 plant extracts were investigated for their inhibition of lipid accumulation in 3T3-L1 cells. Among these 44 extracts examined, crude extracts from 4 natural plant species were active. Salicis Radicis Cortex had the highest fat inhibitory activity, whereas Rubi Fructus, Corni Fructus, and Geranium nepalense exhibited fat inhibitory capacity higher than 30% at 100 μg/mL in 3T3-L1 adipocytes, suggesting anti-obesity activity. These results suggest that four potent plant extracts might be of therapeutic interest with respect to the treatment of obesity.

  17. 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.

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

    Science.gov (United States)

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

    2016-07-19

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

  19. PHYTOCHEMICAL SCREENING AND ANTIBACTERIAL ACTIVITY OF STACHYTARPHETA INDICA

    Directory of Open Access Journals (Sweden)

    H.N. Krishna Kumar*, S.D.Preethi, E. Chandana and Jyoti Bala Chauhan

    2012-01-01

    Full Text Available Phytochemical screening and antibacterial activity of aqueous and methanolic root extracts of Stachytarpheta indica Vahl. was assessed. Phytochemical analysis revealed the presence of flavonoids, terpenoides, tannins and reducing sugars. The antibacterial properties of both the aqueous and methanolic extracts were studied against clinically important bacteria viz., Escherichia coli, Bacillus cereus, Pseudomonas aeruginosa and Enterobacter aerogens by disc diffusion method. The aqueous extract showed significant activity against all the presently investigated species of bacteria which is comparable with standard antibiotic streptomycin. At the concentrations of 50-100µg /disc, aqueous extract showed significant zone of inhibition against E. coli, (14 mm, B. cereus (13 mm, P. aeruginosa, (17 mm, and E. aerogens (7 mm. Minimum Inhibitory Concentration (MIC and Minimum Bactericidal Concentration (MBC have been determined. The MIC values observed was 20, 30, 5 and 25µg/ml (for aqueous extract and 40, 35, 20 and 30µg/ml (for methanolic extract against E. coli, B. cereus, P. aeruginosa, and E. aerogens respectively. Further isolation of active compound responsible for the activity could be the potential sources of new antimicrobial agents.

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

    Institute of Scientific and Technical Information of China (English)

    熊国兵; 王寓; 邱明星

    2015-01-01

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

  1. Screening of antimutagenicity via antioxidant activity in Cuban medicinal plants.

    Science.gov (United States)

    Ramos, A; Visozo, A; Piloto, J; García, A; Rodríguez, C A; Rivero, R

    2003-08-01

    The reducing activity on the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, z.rad;OH radical scavenging potential, in vitro inhibition of lipid peroxidation and modulation of mutagenicity induced by ter-butyl hydroperoxide (TBH) in Escherichia coli were sequentially screened in 45 species of plants used with medicinal purposes in Cuba, in a search for antioxidant agents which protect DNA against oxidative stress.Five species, e.g. Tamarindus indica L., Lippia alba L., Pimenta dioica (L.) Merr, Rheedia aristata Griseb. and Curcuma longa L. displayed IC(50)essential oil of Pimenta dioica, also inhibited oxidative mutagenesis by TBH in Escherichia coli, at concentrations ranging from 150 to 400 micro g/plate.

  2. Phytochemical Screening and Aphrodisiac Activity of Asparagus racemosus

    Directory of Open Access Journals (Sweden)

    Javeed Ahmed Wani

    2011-04-01

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

  3. 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.

  4. 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.

  5. Chemogenomics driven discovery of endogenous polyketide anti-infective compounds from endosymbiotic Emericella variecolor CLB38 and their RNA secondary structure analysis

    Science.gov (United States)

    Yashavantha Rao, H. C.; Rakshith, Devaraju; Harini, Ballagere Puttaraju; Gurudatt, Doddahosuru Mahadevappa; Satish, Sreedharamurthy

    2017-01-01

    In the postgenomic era, a new strategy for chemical dereplication of polyketide anti-infective drugs requires novel genomics and chromatographic strategies. An endosymbiotic fungal strain CLB38 was isolated from the root tissue of Combretum latifolium Blume (Combretaceae) which was collected from the Western Ghats of India. The isolate CLB38 was then identified as Emericella variecolor by its characteristic stellate ascospores culture morphology and molecular analysis of ITS nuclear rDNA and intervening 5.8S rRNA gene sequence. ITS2 RNA secondary structure modeling clearly distinguished fungal endosymbiont E. variecolor CLB38 with other lifestyles in the same monophyletic clade. Ethyl acetate fraction of CLB38 explored a broad spectrum of antimicrobial activity against multidrug resistant pathogens. Biosynthetic PKS type-I gene and chromatographic approach afford two polyketide antimicrobial compounds which identified as evariquinone and isoindolones derivative emerimidine A. MIC of purified compounds against test microorganisms ranged between 3.12 μg/ml and 12.5 μg/ml. This research highlights the utility of E. variecolor CLB38 as an anticipate source for anti-infective polyketide metabolites evariquinone and emerimidine A to combat multidrug resistant microorganisms. Here we demonstrates a chemogenomics strategy via the feasibility of PKS type-I gene and chromatographic approach as a proficient method for the rapid prediction and discovery of new polyketides compounds from fungal endosymbionts. PMID:28245269

  6. 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.

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

    Energy Technology Data Exchange (ETDEWEB)

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

    2013-05-15

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

  8. 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

  9. 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.

  10. Screening culture filtrates of fungi for activity against Tylenchulus semipenetrans

    Energy Technology Data Exchange (ETDEWEB)

    Verdejo-Lucas, S.; Viera, A.; Stchigel, A. M.; Sorribas, F. J.

    2009-07-01

    Culture filtrates of 20 fungi isolated from citrus soils were screened for their activity against Tylenchulus semipenetrans in both in vitro and greenhouse tests. The filtrates of Talaromyces cyanescens (isolates 2-4 and 2-5), Paecilomyces lilacinus, Chaetomium robustum, Acremonium strictum, Engyodontium album, Myrothecium verrucaria, Emericella rugulosa, and Tarracomyces gigaspora consistently inhibited the motility of second-stage juveniles at various concentrations of the filtrate. Dose-response models were used to determine the filtrate concentration required to inhibit the motility of 50% of the juveniles (CI50). The culture filtrate of P. lilacinus showed the highest activity with a CI50 value of 58% that differed from that of C. robustum (CI50 = 68%), and A. strictum CI50 = 82%. The culture filtrates of P. lilacinus, E. album, and T. cyanescens 2-5 maintained their activity when autoclaved at 120 degree centigrade for 20 min. The autoclaved filtrate of T. cyanescens 2-4 was more effective at inhibiting juvenile motility (CI50 = 28%) than that of T. cyanescens 2-5 (CI50 = 80%), C. robustum (CI50 = 72 %) and P. lilacinus (CI50 = 72%). The culture filtrate of T. cyanescens 2-4 also inhibited egg hatching. Nematode reproduction on Cleopatra mandarin and Carrizo citrange were respectively reduced by the culture filtrate of P. lilacinus and the autoclaved filtrate of T. cyanescens 2-4. These results support the hypothesis that soil fungi may contribute to regulate nematode densities by the production of secondary metabolites with nematicidal activity. (Author) 30 refs.

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

    Science.gov (United States)

    Gilmore, Brendan F

    2012-05-01

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

  12. A computational methodology to screen activities of enzyme variants.

    Directory of Open Access Journals (Sweden)

    Martin R Hediger

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

  13. A Computational Methodology to Screen Activities of Enzyme Variants

    CERN Document Server

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

    2012-01-01

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

  14. Screening of estrogenic and antiestrogenic activities from medicinal plants.

    Science.gov (United States)

    Kim, In Gyu; Kang, Se Chan; Kim, Kug Chan; Choung, Eui Su; Zee, Ok Pyo

    2008-01-01

    The medicinal plant extracts commercially used in Asia were screened for their estrogenic and antiestrogenic activities in a recombinant yeast system featuring both a human estrogen receptor (ER) expression plasmid and a reporter plasmid. Pueraria lobata (flower) had the highest estrogenic relative potency (RP, 7.75×10(-3); RP of 17β-estradiol=1), followed by Amomum xanthioides (1.25×10(-3)). Next potent were a group consisting of Glycyrrhiza uralensis, Zingiber officinale, Rheum undulatum, Curcuma aromatica, Eriobotrya japonica, Sophora flavescens, Anemarrhena asphodeloides, Polygonum multiflorum, and Pueraria lobata (root) (ranging from 9.5×10(-4) to 1.0×10(-4)). Least potent were Prunus persica, Lycoppus lucidus, and Adenophora stricta (ranging from 9.0×10(-5) to 8.0×10(-5)). The extracts exerting antiestrogenic effects, Cinnamomum cassia and Prunus persica, had relative potencies of 1.14×10(-3) and 7.4×10(-4), respectively (RP of tamoxifen=1). The solvent fractions from selected estrogenic or antiestrogenic herbs had higher estrogenic relative potencies, with their RP ranging from 9.3×10(-1) to 2.7×10(-4) and from 8.2×10(-1) to 9.1×10(-3), respectively. These results support previous reports on the efficacy of Oriental medicinal plants used or not used as phytoestrogens for hormone replacement therapy.

  15. Direct screening of libraries of yeast clones for alpha-amylase activity on raw starch hydrolysis.

    Science.gov (United States)

    Wong, Dominic W S; Batt, Sarah B; Lee, Charles C; Robertson, George H

    2003-10-01

    High-throughput screening for high-activity barley alpha-amylase mutants expressed in Saccharomyces cerevisiae is hampered by the interference of reducing agents, particularly the glucose used in yeast growth media. The present investigation employed colorimetric and chemiluminescent detection systems that enable direct and rapid screening of activities on raw starch substrate. Active clones could be separated into two groups, based on high total activity or high specific activity.

  16. Identification and characterization of PERK activators by phenotypic screening and their effects on NRF2 activation.

    Directory of Open Access Journals (Sweden)

    Wensheng Xie

    Full Text Available Endoplasmic reticulum stress plays a critical role to restore the homeostasis of protein production in eukaryotic cells. This vital process is hence involved in many types of diseases including COPD. PERK, one branch in the ER stress signaling pathways, has been reported to activate NRF2 signaling pathway, a known protective response to COPD. Based on this scientific rationale, we aimed to identify PERK activators as a mechanism to achieve NRF2 activation. In this report, we describe a phenotypic screening assay to identify PERK activators. This assay measures phosphorylation of GFP-tagged eIF2α upon PERK activation via a cell-based LanthaScreen technology. To obtain a robust assay with sufficient signal to background and low variation, multiple parameters were optimized including GFP-tagged eIF2α BacMam concentration, cell density and serum concentration. The assay was validated by a tool compound, Thapsigargin, which induces phosphorylation of eIF2α. In our assay, this compound showed maximal signal window of approximately 2.5-fold with a pEC50 of 8.0, consistent with literature reports. To identify novel PERK activators through phosphorylation of eIF2α, a focused set of 8,400 compounds was screened in this assay at 10 µM. A number of hits were identified and validated. The molecular mechanisms for several selected hits were further characterized in terms of PERK activation and effects on PERK downstream components. Specificity of these compounds in activating PERK was demonstrated with a PERK specific inhibitor and in PERK knockout mouse embryonic fibroblast (MEF cells. In addition, these hits showed NRF2-dependent anti-oxidant gene induction. In summary, our phenotypic screening assay is demonstrated to be able to identify PERK specific activators. The identified PERK activators could potentially be used as chemical probes to further investigate this pathway as well as the link between PERK activation and NRF2 pathway activation.

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

    Science.gov (United States)

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

    2014-01-01

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

  18. Screening of anticancer activity from agarwood essential oil

    Directory of Open Access Journals (Sweden)

    Yumi Zuhanis Has-Yun Hashim

    2014-01-01

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

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

    Science.gov (United States)

    Kopcakova, Jaroslava; Dankulincova Veselska, Zuzana; Madarasova Geckova, Andrea; 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 cross-sectional study from four European countries (n = 13,800, mean age = 14.4, 49.4% boys). We explored the association of perceived environment (e.g., “There are other children nearby home to go out and play with”) with physical activity and screen-based activities using a binary logistic regression model adjusted for age, gender, family affluence and country. Results: An environment perceived as activity-friendly was associated with higher odds that adolescents meet recommendations for physical activity (odds ratio (OR) for one standard deviation (SD) change = 1.11, 95% confidence interval (CI) 1.05–1.18) and lower odds for excessive screen-based activities (OR for 1 SD better = 0.93, 95% CI 0.88–0.98). Conclusions: Investment into an activity-friendly environment may support the promotion of active life styles in adolescence. PMID:28054953

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

    Directory of Open Access Journals (Sweden)

    Jaroslava Kopcakova

    2017-01-01

    Full Text Available 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 cross-sectional study from four European countries (n = 13,800, mean age = 14.4, 49.4% boys. We explored the association of perceived environment (e.g., “There are other children nearby home to go out and play with” with physical activity and screen-based activities using a binary logistic regression model adjusted for age, gender, family affluence and country. Results: An environment perceived as activity-friendly was associated with higher odds that adolescents meet recommendations for physical activity (odds ratio (OR for one standard deviation (SD change = 1.11, 95% confidence interval (CI 1.05–1.18 and lower odds for excessive screen-based activities (OR for 1 SD better = 0.93, 95% CI 0.88–0.98. Conclusions: Investment into an activity-friendly environment may support the promotion of active life styles in adolescence.

  1. Phytochemical Screening and Pharmacological Activities of Entada Scandens seeds

    Directory of Open Access Journals (Sweden)

    S K Dey

    2013-03-01

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

  2. Evaluation of new anti-infective drugs for the treatment of cholera. Infectious Diseases Society of America and the Food and Drug Administration.

    Science.gov (United States)

    Corrado, M L; DuPont, H L; Cooperstock, M; Fekety, R; Murray, D M

    1992-11-01

    Cholera is an acute gastrointestinal infection caused by Vibrio cholerae. It is characterized by watery diarrhea that may lead to massive fluid loss, which in turn may result in hypotension, shock, and death within hours. Key to the treatment of cholera is fluid replacement. Anti-infective therapy decreases the severity and duration of diarrhea and the duration of shedding of V. cholerae. Enrolled patients should have diarrhea that is moderate to severe and a culture that ultimately yields V. cholerae. A prospective, randomized, active-controlled clinical trial is preferred. Studies should be double-blinded or evaluator-blinded. The rapidity with which the organism is eliminated from stool may be assessed. Both clinical and microbiological outcome should be determined. Assessment of microbiological eradication is paramount, since fluid replacement may suffice for treatment of signs and symptoms.

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

    DEFF Research Database (Denmark)

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

    2013-01-01

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

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

    Science.gov (United States)

    Bosmans, L; De Bruijn, I; De Mot, R; Rediers, H; Lievens, B

    2016-08-01

    Agar-based screening assays are the method of choice when evaluating antagonistic potential of bacterial biocontrol-candidates against pathogens. We showed that when using the same medium, but different agar compositions, the activity of a bacterial antagonist against Agrobacterium was strongly affected. Consequently, results from in vitro screenings should be interpreted cautiously.

  5. Fabrication of drug-loaded anti-infective guided tissue regeneration membrane with adjustable biodegradation property.

    Science.gov (United States)

    Xue, Jiajia; Shi, Rui; Niu, Yuzhao; Gong, Min; Coates, Phil; Crawford, Aileen; Chen, Dafu; Tian, Wei; Zhang, Liqun

    2015-11-01

    For guided tissue regeneration (GTR) membrane, synchronization of the membrane biodegradation rate and tissue regeneration rate is important. Besides, the major reason for GTR membrane failure in clinical application is infection which can be prevented by loading anti-bacterial drug. To realize the consistency in membrane degradation rate and tissue regeneration rate of the anti-infective membrane, we developed metronidazole-loaded electrospun poly(ɛ-caprolactone)-gelatin nanofiber membranes with different poly(ɛ-caprolactone)/gelatin ratios (95:5, 90:10, 80:20, 70:30, 60:40, and 50:50). Homogeneous nanofibers were successfully fabricated. The mechanical strength of the membranes increased with the poly(ɛ-caprolactone) content, while the hydrophilicity decreased. The controlled and sustained release of metronidazole from all the membranes prevented the colonization of anaerobic bacteria. At all poly(ɛ-caprolactone)/gelatin ratios, all the membranes presented good biocompatibility while the increase of gelatin content resulted in enhanced cell adhesion and proliferation. Subcutaneous implantation in rabbits for 8 months demonstrated that all the membranes showed good biocompatibility without infection. Both in vitro and in vivo results showed that the biodegradation rate of the membranes was accelerated with the increase of gelatin content. The biodegradation rate and biocompatibility of the membranes can be adjusted by changing the PCL/gelatin ratio. The optimal membrane can be chosen based on the patient and tissue type to realize the synchronization of membrane degradation with tissue regeneration for the best treatment effect.

  6. 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.

  7. Phytochemical Screening and Aphrodisiac Activity of Asparagus racemosus

    OpenAIRE

    Javeed Ahmed Wani; Achur, Rajeshwara N.; 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...

  8. 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

    2017-01-01

    Abstract Objective To assess the cost–effectiveness of the tuberculosis screening activities currently funded by the Flemish government in Flanders, Belgium. Methods 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. Findings 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. Conclusion 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. PMID:28053362

  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. 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.

  11. Validity of "sputtering and re-condensation" model in active screen cage plasma nitriding process

    Science.gov (United States)

    Saeed, A.; Khan, A. W.; Jan, F.; Abrar, M.; Khalid, M.; Zakaullah, M.

    2013-05-01

    The validity of "sputtering and re-condensation" model in active screen plasma nitriding for nitrogen mass transfer mechanism is investigated. The dominant species including NH, Fe-I, N2+, N-I and N2 along with Hα and Hβ lines are observed in the optical emission spectroscopy (OES) analysis. Active screen cage and dc plasma nitriding of AISI 316 stainless steel as function of treatment time is also investigated. The structure and phases composition of the nitrided layer is studied by X-ray diffraction (XRD). Surface morphology is studied by scanning electron microscopy (SEM) and hardness profile is obtained by Vicker's microhardness tester. Increasing trend in microhardness is observed in both cases but the increase in active screen plasma nitriding is about 3 times greater than that achieved by dc plasma nitriding. On the basis of metallurgical and OES observations the use of "sputtering and re-condensation" model in active screen plasma nitriding is tested.

  12. Identification of mangiferin as a potential Glucokinase activator by structure-based virtual ligand screening.

    Science.gov (United States)

    Min, Qiuxia; Cai, Xinpei; Sun, Weiguang; Gao, Fei; Li, Zhimei; Zhang, Qian; Wan, Luo-Sheng; Li, Hua; Chen, Jiachun

    2017-03-20

    The natural product mangiferin (compound 7) has been identified as a potential glucokinase activator by structure-based virtual ligand screening. It was proved by enzyme activation experiment and cell-based assays in vitro, with potency in micromolar range. Meanwhile, this compound showed good antihyperglycemic activity in db/db mice without obvious side effects such as excessive hypoglycaemia.

  13. A straightforward ninhydrin-based method for collagenase activity and inhibitor screening of collagenase using spectrophotometry.

    Science.gov (United States)

    Zhang, Yanfang; Fu, Yun; Zhou, Sufeng; Kang, Lixia; Li, Changzheng

    2013-06-01

    Currently protease assay kits, requiring substrate that is either radiolabeled or fluorescence labeled and specialized instruments, are all expensive. A simple, reliable assay of protease activity and its inhibitor screening for general laboratory is rare. Here we demonstrated a straightforward ninhydrin-based method for assay of collagenase activity and its inhibitor screening using spectrophotometry. In the method, without multistep sample treatments and substrate labeling, the hydrolytic products were directly traced by ninhydrin. The method is expected to be suitable for not only the assay of collagenase activity but also the others matrix metalloproteinases activities, and can be used for kinetic study.

  14. Evaluation of global, photosynthetically active radiation and diffuse radiation transmission of agricultural screens

    Energy Technology Data Exchange (ETDEWEB)

    Romero-Gamez, M.; Suarez-Rey, E. M.; Castilla, N.; Soriano, T.

    2012-11-01

    Transmittance of a material depends on the type of radiation impinging on the material (direct or diffuse), the angle of incidence of the sun's rays (in direct radiation conditions) and the structure and characteristics of the material itself. The aim of this study was to evaluate the performance of nine agricultural screens of different densities, colours, thread diameters and porosities. A simple metal frame was used to quantify global, diffuse and photosynthetically active radiation (PAR) transmission to determine their transmittance values (as a function of the incidence angle of solar rays in direct radiation conditions) for global radiation and PAR, as well as the diffuse radiation transmitted characteristics of the screens (ratio of diffuse radiation to global radiation transmitted by screens). Non-coloured (translucent) screens contributed to a higher and more efficient proportion of diffuse radiation (Di/Gi {approx} 90%). The green screen behaved similarly to the non-coloured 20 × 10 type as far as global radiation was concerned, although the PAR transmittance values were lower (up to 12.4% at 15°). Variation in transmission according to diameter and density of the threads was greatest in the black screens. The non-coloured-thread screens may be the best option for maximising the transmission of diffuse radiation and the 6 × 6 green screen for vegetables cultivation during the summer in inland areas with latitudes close to 36degree N. (Author) 43 refs.

  15. Screening for fibrinolytic activity in eight Viperid venoms.

    Science.gov (United States)

    Ramírez, M S; Sánchez, E E; García-Prieto, C; Pérez, J C; Chapa, G R; McKeller, M R; Ramírez, R; De Anda, Y

    1999-09-01

    Snake venoms contain direct-acting fibrinolytic metalloproteinases (MMP) that could have important applications in medicine. Fibrinolytic enzymes isolated from venom can induce in vitro clot lysis by directly acting on a fibrin clot. The most ideal fibrinolytic enzyme would have high affinity for clots, dissolve clots directly without causing hemorrhage, and would not be neutralized in vivo by endogenous metalloproteinase inhibitors. The purpose of this study was to compare DEAE/HPLC venom profiles from Viperid snakes and identify fractions that contain fibrinolytic activity with no hemorrhagic activity and are not neutralized by animal sera. The sera selected were from four (Virginia opossum, Gray woodrat, Mexican ground squirrel, and Hispid cottonrat) animals known to neutralize hemorrhagic activity in snake venoms. Nineteen fractions from the Viperid venoms had fibrinolytic activity. Agkistrodon venom fractions contained the highest specific fibrinolytic activities. A. piscivorus leucostoma fraction 4 contained a high specific fibrinolytic activity, no hemorrhagic activity, and the fibrinolytic activity was not neutralized by the proteinase inhibitors of the four animal sera. A. contortrix laticinctus fraction 1 also had a high specific fibrinolytic activity and no hemorrhagic activity. However, the fibrinolytic activity was neutralized by Didelphis virginiana (Virginia opossum) serum.

  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. 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.

  18. 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.

    Bacterial resistance to existing antibiotics has led to the search for new therapeutic agents. With this aim, we have evaluated antimicrobial activity of extracts prepared from forty species of marine organisms belonging to different phyla...

  19. Screening of flocculant-producing microorganisms and flocculating activity

    Institute of Scientific and Technical Information of China (English)

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

    2004-01-01

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

  20. Antitubercular activity and phytochemical screening of selected medicinal plants

    Directory of Open Access Journals (Sweden)

    Rajandeep Kaur

    2015-03-01

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

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

    NARCIS (Netherlands)

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

    2006-01-01

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

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

    Science.gov (United States)

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

  3. Screening of Uruguayan plants for deterrent activity against insects.

    Science.gov (United States)

    Castillo, Lucía; González-Coloma, Azucena; González, Andrés; Díaz, Martina; Santos, Estela; Alonso-Paz, Eduardo; Bassagoda, María Julia; Rossini, Carmen

    2009-01-01

    We evaluated the anti-insectan activity of extracts from different vegetative parts of ten plant species native to Uruguay. The selected plants belong to five families: Bignoniaceae: Clytostoma callistegioides, Dolichandra cynanchoides, Macfadyena unguis-cati; Sapindaceae: Dodonaea viscosa, Allophylus edulis, Serjania meridionalis; Lamiaceae: Salvia procurrens, Salvia guaranitica; Solanaceae: Lycium cestroides; and Phytolaccaceae: Phytolacca dioica. The extracts were evaluated in independent bioassays against four insect pests and one beneficial insect. Aphid settling inhibition was evaluated with a grass specialist, Rhopalosiphum padi, and a feeding generalist, Myzus persicae (both Hemiptera: Aphididae). Antifeedant activity was tested with adults of the specialist Epilachna paenulata (Coleoptera: Coccinellidae) and larvae of the generalist Spodoptera littoralis (Lepidoptera: Noctuidae). Finally, contact toxicity was assessed with honey bees, Apis mellifera (Hymenoptera: Apidae). Strong settling inhibition (SI) activity (expressed as %SI, where 100% means complete inhibition by the extract) was found only for the twig extracts of A. edulis (Sapindaceae) against M. persicae (% SI = 77 +/- 4). Antifeedant activity (expressed as % of feeding reduction (FR), where 100% means no consumption on extract-treated diet) against E. paenulata was significant for the leaf extracts of L. cestroides (Solanaceae) (% FR = 100 +/- 0) as well as of all Bignoniaceae and Sapindaceae species. No extracts were active against S. littoralis larvae, and most of them were innocuous to honey bees, with the exception of L. cestroides and S. meridionalis leaf extracts.

  4. [Antitumor components screening of Stellera chamaejasme L. under the case of discrete distribution of active data].

    Science.gov (United States)

    Yang, Qian-Xu; Cheng, Meng-Chun; Wang, Li; Kan, Xiao-Xi; Zhu, Xiao-Xin; Xiao, Hong-Bin

    2014-06-01

    This is to report the screening, extracting and validating antitumor components and compounds from Stellera chamaejasme L. under the case of discrete distribution of active data. In this work, different components from Stellera chamaejasme L. were collected by HPD macroporous resin and polyamide resin column, and their antitumor activity on A549 were tested by MTT assay. Activity results indicate that activity of components at 30-39 min is more potent than that of Stellera chamaejasme L. extract, and the activity of components at 33.97 min is equivalent to positive drug, cis-platinum at 100 microg x mL(-1), but with totally different mode of action. Under the case of discrete activity, the weight analysis is capable of screening active components and compounds from natural products.

  5. Posture, muscle activity and muscle fatigue in prolonged VDT work at different screen height settings.

    Science.gov (United States)

    Seghers, Jan; Jochem, Arnaud; Spaepen, Arthur

    2003-06-10

    With the increasing use of video display terminals (VDTs), there is growing concern over the corresponding increase in the number of health problems reported. Although much research has focused on identifying the optimal screen height, there is to date no consensus. This study aimed to investigate the effect of prolonged (89 min) VDT work at four different screen heights on head-neck posture, muscle activity and the development of muscle fatigue. The results show that lowering screen height, starting from 15 cm above the baseline (i.e. top of the screen level with eye height while sitting), decreased the ear-eye angle, increased the viewing angle, increased the viewing angle relative to the ear-eye line, and increased the muscle activity of the neck extensor muscles. There were also some significant time effects on postural angles and muscle activity. In this study there were only rare occurrences of muscle fatigue, defined as a simultaneous increase in EMG amplitude and a shift of the EMG power spectrum to lower frequencies. Muscle activity increased significantly in some muscles and for certain screen heights.

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

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    Mazandarani Masoumeh

    2015-04-01

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

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

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

    2012-02-01

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

  8. Screening for antibacterial and antibiofilm activities in Astragalus angulosus

    Science.gov (United States)

    Kanaan, Hussein; El-Mestrah, Majid; Sweidan, Alaa; As-Sadi, Falah; Bazzal, Ali Al; Chokr, Ali

    2017-01-01

    Aim: In a search for finding novel therapeutic agents, extracts from an endemic Lebanese plant, Astragalus angulosus, were evaluated for their potential in-vitro antibacterial and antibiofilm activities against three Gram-positive bacterial strains; Staphylococcus epidermidis (CIP444), Staphylococcus aureus (ATCC25923), and Enterococcus faecalis (ATCC29212); in addition to two Gram-negative strains, Escherichia coli (ATCC35218) and Pseudomonas aeruginosa (ATCC27853). Materials and Methods: The plant was collected in April of 2013 and 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 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 S. 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. 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. PMID:28163960

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

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    Akram Astani

    2011-01-01

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

  10. 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.

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

    Science.gov (United States)

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

    2016-09-20

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

  12. Screening of cetirizine for analgesic activity in mice

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    Priya M

    2013-04-01

    Full Text Available Background: Pain is the most common symptom for which patients approach doctors. We have multitude of drugs for pain relief, but they have serious side effects ranging from peptic ulcer (e.g. NSAIDs to renal failure. The other group, opioids have well known side effects ranging from sedation to drug dependence. So a search for a drug for analgesia with high therapeutic effect and fewer side effects will be a boon for the patients. The objective of this study was to find whether cetirizine, a second generation antihistaminic drug, has got any analgesic activity in mice. Methods: Ten adult albino mice weighing 20-30 grams of either sex were randomized to two groups (n=5. Group I: control group (Treated with solvent 0.1 ml/kg, Group II: Test group (Cetirizine 1mg/kg. All drugs were given orally. The analgesic activity was evaluated by using tail flick, tail immersion and tail clip methods. Reaction time of animals to pain sensation before and after Cetirizine administration were noted at 0, 15, 30, 60 and 90 minutes time intervals respectively on Day 1, 3, 5, 7, 10. Results: Mean reaction time was expressed as Mean±SEM, and one way ANOVA was used to assess statistical significance. Cetirizine was found to have statistically significant analgesic effect in mice and time dependent increase in analgesic effect were observed in all three pain models and maximum analgesic activity was observed at 60 minutes (p<0.001 after drug administration. Conclusions: Through this study, Cetirizine, a second generation antihistamine, is found to have significant analgesic activity in mice. This effect has to be studied further elaborately in animals as well as in humans. [Int J Basic Clin Pharmacol 2013; 2(2.000: 187-192

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

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    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.

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

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    M. P. SINHA

    2013-01-01

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

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

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    Catherine Moorwood

    Full Text Available BACKGROUND: 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. METHODOLOGY/PRINCIPAL FINDINGS: 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. CONCLUSIONS/SIGNIFICANCE: 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.

  16. Screening of antidiabetic and antioxidant activities of medicinal plants

    Institute of Scientific and Technical Information of China (English)

    Amal Bakr Shori

    2015-01-01

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

  17. A screening study of xylitol binding in vitro to activated charcoal.

    Science.gov (United States)

    Cope, R B

    2004-12-01

    Ingestion of foods containing the sweetener xylitol by dogs results in a significant, and often sustained, insulin-mediated hypoglycemic crisis. The efficacy of activated charcoal for gastrointestinal decontamination following xylitol ingestion is unknown. This screening study examined the effect of pH and incubation time on the in vitro binding of xylitol to activated charcoal. The mean percentage activated charcoal binding ranged between 8 and 23%. Mean percentage binding of xylitol at pH 3 was significantly higher (p activated charcoal slurry. These results suggest binding of xylitol to activated charcoal is relatively low; however, activated charcoal administration may still be beneficial in some canine acute oral xylitol exposures.

  18. Cell extraction combined with off-line HPLC for screening active compounds from Coptis chinensis.

    Science.gov (United States)

    Tang, Cheng; Wu, Xiao-Dan; Yu, Ya-Ming; Duan, Hongquan; Zhou, Jing; Xu, Liang

    2016-04-01

    Cell membrane chromatography is a useful tool for screening active compounds from natural products. As the reason of separation mechanism, traditional cell membrane chromatography could not be used for screening the active compounds absorbed through the cell membrane and influencing the cell signal transduction pathway. In this work, we establish a new method named cell extraction combined with off-line HPLC for screening the compounds penetrating the cell membrane. This is the first time 3 T3-L1 adipocyte culture has been combined with HPLC technology. Compared with other cell membrane chromatography methods, there is good resolution and no further analysis by other chromatographic steps is required. On co-incubating crude extracts of Coptis chinensis with cells and analyzing the compounds extracted by the cells, active compounds such as berberine were detected. Glucose consumption tests showed that berberine could increase glucose consumption by insulin-resistant 3 T3-L1 adipocytes. The levels of intracellular berberine correlated with its activity. The results indicate that the developed method could be an alternative method for screening active compounds from natural products.

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

    Science.gov (United States)

    Huang, Ruili

    2016-01-01

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

  20. Bacillus subtilis as a tool for screening soil metagenomic libraries for antimicrobial activities.

    Science.gov (United States)

    Biver, Sophie; Steels, Sébastien; Portetelle, Daniel; Vandenbol, Micheline

    2013-06-28

    Finding new antimicrobial activities by functional metagenomics has been shown to depend on the heterologous host used to express the foreign DNA. Therefore, efforts are devoted to developing new tools for constructing metagenomic libraries in shuttle vectors replicatable in phylogenetically distinct hosts. Here we evaluated the use of the Escherichia coli-Bacillus subtilis shuttle vector pHT01 to construct a forest-soil metagenomic library. This library was screened in both hosts for antimicrobial activities against four opportunistic bacteria: Proteus vulgaris, Bacillus cereus, Staphylococcus epidermidis, and Micrococcus luteus. A new antibacterial activity against B. cereus was found upon screening in B. subtilis. The new antimicrobial agent, sensitive to proteinase K, was not active when the corresponding DNA fragment was expressed in E. coli. Our results validate the use of pHT01 as a shuttle vector and B. subtilis as a host to isolate new activities by functional metagenomics.

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

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    A. Vimalavady et al.

    2012-04-01

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

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

    Science.gov (United States)

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

    2016-12-15

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

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

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    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

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

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    Gordon-Larsen Penny

    2007-06-01

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

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

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    Md. Faruk Hasan

    2016-06-01

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

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

    Directory of Open Access Journals (Sweden)

    Carrie Selin

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

  7. 78 FR 38452 - Agency Information Collection (VA Police Officer Pre-Employment Screening Checklist) Activities...

    Science.gov (United States)

    2013-06-26

    ... 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... Management and Budget (OMB) for review and comment. The PRA submission describes the nature of...

  8. 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.

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

    DEFF Research Database (Denmark)

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

    2016-01-01

    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. RESULTS: For neuromuscular hamstring muscle pre...

  10. 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 c

  11. 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

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

    NARCIS (Netherlands)

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

    2002-01-01

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

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

    Directory of Open Access Journals (Sweden)

    Dr. D. Gopala Krishna

    2013-05-01

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2014-01-01

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

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

    Directory of Open Access Journals (Sweden)

    Christelle Cabrol

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

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

    Institute of Scientific and Technical Information of China (English)

    Emilda Rosmine

    2016-01-01

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

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

    Science.gov (United States)

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

    2015-01-01

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

  18. 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.

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

    Science.gov (United States)

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

    2016-03-01

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

  20. 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.

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

    Directory of Open Access Journals (Sweden)

    Parekh Jigna

    2006-01-01

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

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

    Science.gov (United States)

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

    2005-06-15

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

  3. Disentangling the roles of mammographic screening and HRT in recent breast cancer incidence trends in italy by analyses based on calendar time and time since screening activation.

    Science.gov (United States)

    Crocetti, Emanuele; Buzzoni, Carlotta; Falcini, Fabio; Cortesi, Laura; De Lisi, Vincenzo; Ferretti, Stefano; Tumino, Rosario; Russo, Antonio; Paci, Eugenio

    2010-01-01

    The aim of the study was to evaluate the roles of screening activation and hormone replacement therapy discontinuation on the recent declining breast cancer incidence trends in Italy. We analyzed 41,358 invasive female breast cancers incident during 1991-2004 in six Italian population-based cancer registries. Overall and age-specific incidence trends were evaluated using Joinpoint analysis. In addition to calendar years, data were analyzed on a years-since-screening-activation basis. Annual percentage change of standardized rates was computed. There were statistically significant increasing trends for women 40-44 and 45-49 years that did not change after screening activation. On the contrary, for women 50-69 years old and for those 70+ years, the increasing trends flattened around 2 years after screening activation. The prevalence of hormone replacement therapy use in Italy is and was rather low. In conclusion, the recent tendency toward stabilization observed in Italy for female breast cancer incidence rates in women aged 50 years or more follows the introduction of mammographic screening.

  4. The Effect of Using Dual Screen Computer Panel to the Neck-Shoulder Muscle Activity among Group of Students

    Directory of Open Access Journals (Sweden)

    Shamsul Bahri TAMRIN

    2016-03-01

    Full Text Available Background: Workstation design has shift from using single monitor screen to dual monitor screens, which may impose some impacts towards the muscles activity. This study aimed to determine the effect of using dual monitor screen computer to the neck-shoulder muscle activity among computer user.Method: This experimental study was conducted in 2015 among 28 healthy students in University Malaysia Perlis. The muscle activity of sternocleidomastoid and trapezius were recorded using surface electromyography (sEMG as the participants perform two types of computer task: (1 proofreading task for 10 minutes (2 typing task for 20 minutes in setting; single and dual monitor screens.Results: There was a significant reduction in the median frequency of the left trapezius muscle (t=-2.515, P=0.018. Sternocleidomastoid muscle activity for both sides also showed a significant reduction in the median frequency where right SCM (t=-2.579, P=0.016 and left SCM (t=-2.345, P=0.027. When compared between both setup of screen display, it is showed that dual screen gave a lower trend of muscle activity compared to single screen.Conclusions: Using dual screen may results in increasing the movement frequency and reducing the static strain in the neck-shoulder muscle area. Keywords: Dual monitor screen, Neck-shoulder muscles, Surface electromyography

  5. Syringe test screening of microbial gas production activity: Cases denitrification and biogas formation.

    Science.gov (United States)

    Østgaard, Kjetill; Kowarz, Viktoria; Shuai, Wang; Henry, Ingrid A; Sposob, Michal; Haugen, Hildegunn Hegna; Bakke, Rune

    2017-01-01

    Mass produced plastic syringes may be applied as vessels for cheap, simple and large scale batch culture testing. As illustrated for the cases of denitrification and of biogas formation, metabolic activity was monitored by direct reading of the piston movement due to the gas volume formed. Pressure buildup due to friction was shown to be moderate. A piston pull and slide back routine can be applied before recording gas volume to minimize experimental errors due to friction. Inoculum handling and activity may be conveniently standardized as illustrated by applying biofilm carriers. A robust set of positive as well as negative controls ("blanks") should be included to ensure quality of the actual testing. The denitrification test showed saturation response at increasing amounts of inoculum in the form of adapted moving bed biofilm reactor (MBBR) carriers, with well correlated nitrate consumption vs. gas volume formed. As shown, the denitrification test efficiently screened different inocula at standardized substrates. Also, different substrates were successfully screened and compared at standardized inocula. The biogas potential test showed efficient screening of different substrates with effects of relative amounts of carbohydrate, protein, fat. A second case with CO2 capture reclaimer waste as substrate demonstrated successful use of co-feeding to support waste treatment and how temperature effects on kinetics and stoichiometry can be observed. In total, syringe test screening of microbial gas production seems highly efficient at a low cost when properly applied.

  6. 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

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

    Science.gov (United States)

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

    2015-04-01

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

  8. Comparison of in vitro and in vivo screening models for androgenic and estrogenic activities.

    Science.gov (United States)

    Sonneveld, Edwin; Riteco, Jacoba A C; Jansen, Hendrina J; Pieterse, Bart; Brouwer, Abraham; Schoonen, Willem G; van der Burg, Bart

    2006-01-01

    Identification of nuclear receptor-mediated endocrine activities is important in a variety of fields, ranging from pharmacological and clinical screening, to food and feed safety, toxicological monitoring, and risk assessment. Traditionally animal studies such as the Hershberger and Allen-Doisy tests are used for the assessment of androgenic and estrogenic potencies, respectively. To allow fast analysis of the activities of new chemicals, food additives, and pharmaceutical compounds, high-throughput screening strategies have been developed. Here, a panel of mainly steroidal compounds, screened in different in vitro assays, was compared with two human U2-OS cell line-based CALUX (Chemically Activated LUciferase eXpression) reporter gene assays for androgens (AR CALUX) and estrogens (ERalpha CALUX). Correlations found between the data of these two CALUX reporter gene assays and data obtained with other in vitro screening assays measuring receptor binding or reporter gene activation (CHO cell line-based) were good (correlation coefficients (r2) between 0.54 and 0.76; p vitro and in vivo data (correlation coefficient r2 = 0.46 for the AR CALUX vs. Hershberger assay and r2 = 0.87 for the ERalpha CALUX vs. Allen-Doisy assay). The variations in the results obtained with the reporter gene assays (CALUX vs. CHO cell line based) were relatively small, showing the robustness of these types of assays. Using hierarchical clustering, bioactivity relationships between compounds but also relationships between various bioassays were determined. The in vitro assays were found to be good predictors of in vivo androgenic or estrogenic activity of a range of compounds, allowing prescreen and/or possible reduction of animal studies.

  9. 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.

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

    Science.gov (United States)

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

    2016-10-01

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

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

    Science.gov (United States)

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

    2016-05-01

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

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

    Science.gov (United States)

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

    2015-04-03

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

  13. 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.

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

    Directory of Open Access Journals (Sweden)

    Xavier Vergeese raja

    2012-10-01

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

  15. 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.

  16. 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.

  17. Genetic Screening for Bacterial Mutants in Liquid Growth Media By Fluorescence-Activated Cell Sorting

    Science.gov (United States)

    Abuaita, Basel H.; Withey, Jeffrey H.

    2010-01-01

    Many bacterial pathogens have defined in vitro virulence inducing conditions in liquid media which lead to production of virulence factors important during an infection. Identifying mutants that no longer respond to virulence inducing conditions will increase our understanding of bacterial pathogenesis. However, traditional genetic screens require growth on solid media. Bacteria in a single colony are in every phase of the growth curve, which complicates the analysis and make screens for growth phase-specific mutants problematic. Here, we utilize fluorescence-activated cell sorting in conjunction with random transposon mutagenesis to isolate bacteria grown in liquid media that are defective in virulence activation. This method permits analysis of an entire bacterial population in real time and selection of individual bacterial mutants with the desired gene expression profile at any time point after induction. We have used this method to identify Vibrio cholerae mutants defective in virulence induction. PMID:21094189

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

    OpenAIRE

    Ali M. El-Halawany; Riham Salah El Dine; Mi Hwa Chung; Tsutomu Nishihara; Masao Hattori

    2011-01-01

    Background: There is a growing demand for the discovery of new phytoestrogens to be used as a safe and effective hormonal replacement therapy. Materials and Methods: The methanol extracts of 40 plants from the Egyptian and Thailand folk medicines were screened for their estrogen agonist and antagonist activities. The estrogenic and antiestrogenic effects of the tested extracts were carried out using the yeast two-hybrid assay system expressing ERα and ERβ. In addition, all the extracts were s...

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

    OpenAIRE

    Okoh Anthony I; Aiyegoro Olayinka A

    2010-01-01

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

  20. Quantitative Population Epigenetics in Screening and Development of Regulator-Active Factors of the Farming System

    OpenAIRE

    Stauss, R.

    2013-01-01

    Likewise, index selection based on statistical genetic theory in plant and animal breeding the methodology "Quantitative Population Epigenetics" can be appropriated to improve efficiency in screening and development of regulator-active factors of the farming system for potential to enhance quantitative characters such as yield, standability and resistance to unfavorable environmental influences (e.g., water stress, cold temperatures, disease resistance). For example, as was shown for an ef...

  1. Preliminary phytochemical screening and antioxidant activities of solvent extracts from Daucus crinitus Desf., from Algeria

    OpenAIRE

    Bendiabdellah, Amel; DIB, Mohammed El Amine; Meliani, Nawel; Djabou, Nassim; Allali, Hocine; Tabti, Boufeldja

    2012-01-01

    The presence of natural antioxidant in plants is well known. Plant phenolics constitute one of the major groups of components that act as primary antioxidant free radical terminators. This paper reports the antioxidative activity of methanolic and water extract of Daucus crinitus Desf. Phytochemical screening of the crude extracts of stems/leaves revealed the presence of different kind of chemical groups such as tannin, flavonoids, phenolic acids and coumarins. The amounts of tota...

  2. A review of anti-infective and anti-inflammatory chalcones.

    Science.gov (United States)

    Nowakowska, Zdzisława

    2007-02-01

    Chalcones, considered as the precursors of flavonoids and isoflavonoids, are abundant in edible plants, and have also been shown to display a diverse array of pharmacological activities. The purpose of this review is to provide an overview of the pharmacological activity of synthetic and naturally occurring chalcones. This review is complementary to earlier reviews and covers more recent reports of antimicrobial activity of chalcones (antibacterial and antifungal), as well as antileishmanial, antimalarial, antiviral and anti-inflammatory activities of these compounds.

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

    Science.gov (United States)

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

    2012-01-01

    Due to the inexorable invasion of our hospitals and communities by drug-resistant bacteria, there is a pressing need for novel antibacterial agents. Here we report the development of a sensitive and robust but low-tech and inexpensive high-throughput metabolic screen for novel antibiotics. This screen is based on a colorimetric assay of pH that identifies inhibitors of bacterial sugar fermentation. After validation of the method, we screened over 39,000 crude extracts derived from organisms that grow in the diverse ecosystems of Costa Rica and identified 49 with reproducible antibacterial effects. An extract from an endophytic fungus was further characterized, and this led to the discovery of three novel natural products. One of these, which we named mirandamycin, has broad-spectrum antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Vibrio cholerae, methicillin-resistant Staphylococcus aureus, and Mycobacterium tuberculosis. This demonstrates the power of simple high throughput screens for rapid identification of new antibacterial agents from environmental samples. PMID:22359585

  4. 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.

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

    Science.gov (United States)

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

    2016-09-26

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

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

    NARCIS (Netherlands)

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

    2014-01-01

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

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

    Science.gov (United States)

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

    2014-12-01

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

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

    Science.gov (United States)

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

    2016-04-15

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

  9. Screening of Potential Free Radicals Scavenger and Antibacterial Activities of Purwoceng (Pimpinella alpina Molk)

    Science.gov (United States)

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

    2016-01-01

    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. PMID:27965755

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

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

    Directory of Open Access Journals (Sweden)

    Umer Qadir

    2015-04-01

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

  12. Synthesis and antibacterial activity screening of quaternary ammonium derivatives of triazolyl pyranochromenones

    Indian Academy of Sciences (India)

    PREETI YADAV; BIPUL KUMAR; HEMANT K GAUTAM; SUNIL K SHARMA

    2017-02-01

    A series of quaternary ammonium derivatives of triazolyl pyranochromen-2-ones have been synthesized and characterized; their antibacterial potential were investigated against two gram negative (Pseudomonas aeruginosa and Escherichia coli) and two gram positive bacterial strains (Bacillus cereus and Staphylococcus aureus). In order to develop structure-activity relationship (SAR), the effect of varying the substituent (R) at the C-10 position of pyranochromen-2-one as well as the length of the spacer (n) between the triazolyl pyranochromen-2-ones and quaternary ammonium group, on the antibacterial activity of compoundshas been evaluated. Some of the screened compounds exhibited antibacterial potential against the studied strains in the microgram range.

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

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

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

  14. Toward an objective indexing system for ADHD-screening using children's activity monitoring.

    Science.gov (United States)

    Kam, Hye Jin; Choi, Jong Pil; Park, Rae Woong

    2008-11-06

    Signs of ADHD are discernible in specific situations, and usually assessed according to subjective impressions. We performed a preliminary comparative study from children's activity at a natural classroom environment with 3-axis accelerator for a feasible objective index. From a total of 157 children (7-9 yrs) and clinically diagnosed 24 children out of them, variances in 1-min epoch mean activity had shown significant differences among the subgroups: (1) ADHD=.0194, Other Diseases=.0080, Normal=.0009; (2) ADHD=.0194, non-ADHD=.0057(p1.6G) features among subgroups with the same order (pindexing system for screening ADHD patients.

  15. 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.

  16. An in vitro model for screening estrogen activity of environmental samples after metabolism

    Energy Technology Data Exchange (ETDEWEB)

    Chahbane, N.; Schramm, K.W. [GSF - Forschungszentrum fuer Umwelt und Gesundheit Neuherberg GmbH, Oberschleissheim (Germany). Inst. fuer Oekologische Chemie; Kettrup, A. [Technische Univ. Muenchen, Freising (Germany). Lehrstuhl fuer Oekologische Chemie

    2004-09-15

    For a few years, yeast estrogen assay (YES) was accepted as a reliable and economic model for screening of environmental estrogens. Though the chemicals directly act with estrogen receptor (ER) can be filtered out by this model, there are still chemicals act with ER only after metabolism and some chemicals eliminate their estrogen activities after metabolism. That is to say, their metabolites exert or have stronger estrogen activities than themselves, which can be called bio-activation. In this case, for the lack of the metabolism enzyme system as human and other animals, only the assay with recombinant yeast cells is insufficient. So, it is necessary to combine the YES with metabolism procedure to evaluate the estrogen activities of these chemicals. The most common method used currently for in vitro metabolic activation in mutagenicity testing and also be applied to the estrogen screening field is S-9 mixture. Also, there is an attempt to develop a chemical model for cytochrome P450 as a bio-mimetic metabolic activation system. All these methods can be used as in vitro models for metabolism. Compare with these models, using whole H4II E cells for metabolism is an alternative and with superiorities. It has the excellence of short experiment period as all other in vitro models, but is much more close to the real surroundings as in vivo. Furthermore, the activity of 7-ethoxyresorufin-O-deethylase (EROD) can be easily measured during the whole incubation period for us to discuss the metabolic activities in a quantitative foundation, not only in qualitative. Methoxychlor is one of the chemicals with bio-activation ability. When directly used in the YES, it shows weak estrogen activity. But a main metabolite of methoxychlor, 2,2-bis (p-hydroxyphenyl) - 1,1,1-trichloroethane (HPTE) is a known estrogen mimic. For the long time using methoxychlor as a pesticide and its clear background, it is an ideal chemical to establish this in vitro system.

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

    Science.gov (United States)

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

    2016-07-26

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

  18. [Screening for cardiovascular diseases among teenagers that will engage in sport activities].

    Science.gov (United States)

    Díaz, Franco; Mercado, Carolina; Troncoso, Ivana; Heusser, Felipe; Clavería, Cristián

    2010-02-01

    Promotion of physical activity must be a priority in all modern societies, but there are some persons with medical conditions that can develop serious symptoms associated with sports, that can even be fatal, such as sudden death (SD). Adolescents are the age groups with the higher level of participation in recreation or competitive sports. International studies have demonstrated that approximately 1:250.000 adolescents die during the practice of sports. Of these, 50% had a prodrome 24 hours before the event and 75% had an underlying cardiovascular disease. Therefore, adolescents should be screened for cardiovascular diseases prior to their engagement in sports. This review gives a scientific approach to this issue, usually oversized by mass media. It also analyzes and reports international governmental strategies and practical tools for the clinician that must perform this type of screening.

  19. Computational approaches to screen candidate ligands with anti- Parkinson's activity using R programming.

    Science.gov (United States)

    Jayadeepa, R M; Niveditha, M S

    2012-01-01

    It is estimated that by 2050 over 100 million people will be affected by the Parkinson's disease (PD). We propose various computational approaches to screen suitable candidate ligand with anti-Parkinson's activity from phytochemicals. Five different types of dopamine receptors have been identified in the brain, D1-D5. Dopamine receptor D3 was selected as the target receptor. The D3 receptor exists in areas of the brain outside the basal ganglia, such as the limbic system, and thus may play a role in the cognitive and emotional changes noted in Parkinson's disease. A ligand library of 100 molecules with anti-Parkinson's activity was collected from literature survey. Nature is the best combinatorial chemist and possibly has answers to all diseases of mankind. Failure of some synthetic drugs and its side effects have prompted many researches to go back to ancient healing methods which use herbal medicines to give relief. Hence, the candidate ligands with anti-Parkinson's were selected from herbal sources through literature survey. Lipinski rules were applied to screen the suitable molecules for the study, the resulting 88 molecules were energy minimized, and subjected to docking using Autodock Vina. The top eleven molecules were screened according to the docking score generated by Autodock Vina Commercial drug Ropinirole was computed similarly and was compared with the 11 phytochemicals score, the screened molecules were subjected to toxicity analysis and to verify toxic property of phytochemicals. R Programming was applied to remove the bias from the top eleven molecules. Using cluster analysis and Confusion Matrix two phytochemicals were computationally selected namely Rosmarinic acid and Gingkolide A for further studies on the disease Parkinson's.

  20. A high throughput screen for biomining cellulase activity from metagenomic libraries.

    Science.gov (United States)

    Mewis, Keith; Taupp, Marcus; Hallam, Steven J

    2011-02-01

    Cellulose, the most abundant source of organic carbon on the planet, has wide-ranging industrial applications with increasing emphasis on biofuel production (1). Chemical methods to modify or degrade cellulose typically require strong acids and high temperatures. As such, enzymatic methods have become prominent in the bioconversion process. While the identification of active cellulases from bacterial and fungal isolates has been somewhat effective, the vast majority of microbes in nature resist laboratory cultivation. Environmental genomic, also known as metagenomic, screening approaches have great promise in bridging the cultivation gap in the search for novel bioconversion enzymes. Metagenomic screening approaches have successfully recovered novel cellulases from environments as varied as soils (2), buffalo rumen (3) and the termite hind-gut (4) using carboxymethylcellulose (CMC) agar plates stained with congo red dye (based on the method of Teather and Wood (5)). However, the CMC method is limited in throughput, is not quantitative and manifests a low signal to noise ratio (6). Other methods have been reported (7,8) but each use an agar plate-based assay, which is undesirable for high-throughput screening of large insert genomic libraries. Here we present a solution-based screen for cellulase activity using a chromogenic dinitrophenol (DNP)-cellobioside substrate (9). Our library was cloned into the pCC1 copy control fosmid to increase assay sensitivity through copy number induction (10). The method uses one-pot chemistry in 384-well microplates with the final readout provided as an absorbance measurement. This readout is quantitative, sensitive and automated with a throughput of up to 100X 384-well plates per day using a liquid handler and plate reader with attached stacking system.

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

    Directory of Open Access Journals (Sweden)

    Yi Wang

    2016-01-01

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

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

    Science.gov (United States)

    Wang, Yi; Liang, Xinying; Chen, Yaqi; Zhao, Xiaoping

    2016-01-01

    Sirtuin type 1 (SIRT1) belongs to the family of NAD+ dependent histone deacetylases and plays a critical role in cellular metabolism and response to oxidative stress. Traditional Chinese medicines (TCMs), as an important part of natural products, have been reported to exert protective effect against oxidative stress in mitochondria. In this study, we screened SIRT1 activators from TCMs and investigated their activities against mitochondrial damage. 19 activators were found in total by in vitro SIRT1 activity assay. Among those active compounds, four compounds, ginsenoside Rb2, ginsenoside F1, ginsenoside Rc, and schisandrin A, were further studied to validate the SIRT1-activation effects by liquid chromatography-mass spectrometry and confirm their activities against oxidative damage in H9c2 cardiomyocytes exposed to tert-butyl hydroperoxide (t-BHP). The results showed that those compounds enhanced the deacetylated activity of SIRT1, increased ATP content, and inhibited intracellular ROS formation as well as regulating the activity of Mn-SOD. These SIRT1 activators also showed moderate protective effects on mitochondrial function in t-BHP cells by recovering oxygen consumption and increasing mitochondrial DNA content. Our results suggested that those compounds from TCMs attenuated oxidative stress-induced mitochondrial damage in cardiomyocytes through activation of SIRT1. PMID:26981165

  3. PRENYLATED BENZOIC ACID DERIVATIVES FROM PIPER SPECIES AS SOURCE OF ANTI-INFECTIVE AGENTS

    OpenAIRE

    2012-01-01

    A number of prenylated benzoic acids derivatives with interesting biological activities have been previously isolated and characterized from different species of piperaceae family. Several Piper species contained structurally similar compounds with diverse biological activities such as anti-bacterial, anti-fungal, insecticidal as well as anti-parasitic all of which produces compounds that can be classified as prenylated benzoic acid derivatives. Piper sp has proven to serve as a source of pot...

  4. 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.

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

    Directory of Open Access Journals (Sweden)

    S.Nethaji

    2013-12-01

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

  6. SPLICEFINDER - a fast and easy screening method for active protein trans-splicing positions.

    Directory of Open Access Journals (Sweden)

    Joachim Zettler

    Full Text Available Split intein enabled protein trans-splicing (PTS is a powerful method for the ligation of two protein fragments, thereby paving the way for various protein modification or protein function control applications. PTS activity is strongly influenced by the amino acids directly flanking the splice junctions. However, to date no reliable prediction can be made whether or not a split intein is active in a particular foreign extein context. Here we describe SPLICEFINDER, a PCR-based method, allowing fast and easy screening for active split intein insertions in any target protein. Furthermore we demonstrate the applicability of SPLICEFINDER for segmental isotopic labeling as well as for the generation of multi-domain and enzymatically active proteins.

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

    Directory of Open Access Journals (Sweden)

    Márcia Thaís Pochapski

    2011-01-01

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

  8. 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

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

    Institute of Scientific and Technical Information of China (English)

    刘保池; 张磊; 李垒; 司炎辉; 宋言峥; 赵中辛

    2012-01-01

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

  10. Combinatorial Screening Identifies Novel Promiscuous Matrix Metalloproteinase Activities that Lead to Inhibition of the Therapeutic Target IL-13

    NARCIS (Netherlands)

    Urbach, Carole; Gordon, Nathaniel C; Strickland, Ian; Lowne, David; Joberty-Candotti, Cathy; May, Richard; Herath, Athula; Hijnen, DirkJan; Thijs, Judith L; Bruijnzeel-Koomen, Carla A; Minter, Ralph R; Hollfelder, Florian; Jermutus, Lutz

    2015-01-01

    The practical realization of disease modulation by catalytic degradation of a therapeutic target protein suffers from the difficulty to identify candidate proteases, or to engineer their specificity. We identified 23 measurable, specific, and new protease activities using combinatorial screening of

  11. DROSOPHILA MELANOGASTER MG. AS THE TEST-OBJECT FOR SCREENING XENOBIOTICS ON ACARICIDAL ACTIVITY

    Directory of Open Access Journals (Sweden)

    Belokon S.V.

    2015-04-01

    Full Text Available The development of new effective test systems for screening xenobiotics on biological activity, including its possible harmful influence on the organism is the modern challenge. Test systems of eukaryotic origin are needed for testing of xenobiotics on their gonadotoxical, embryotoxic, teratogenic, and carcinogenic effects. Such testing should include the monitoring of genetic effects of bioactive compounds and the possible mutagenic effect. The Drosophila melanogaster Mg. is very convenient test object as a classical genetics object, for which the genome is fully sequenced. It is convenient and easy to find out the frequency of crossingover in different parts of the genome, and study the key indicators of vitality and ontogenetic adaptation (fertility, longevity, survival under stress conditions, etc. on Drosophila. The crossover frequency, in our opinion, can be an integral factor for the general state of genotype.so we could use the mark of genetic recombination frequency as one of the indicators of the impact of xenobiotics. In this study we examined the possibility of using Drosophila melanogaster Mg. (Diptera, Drosophilidae as a test object for screening xenobiotics on acaricidal activity. Sensitivity of flies to acaricides piridaben (Sanmayt and proparhit (Omayt was studied by their fitness, longevity, fertility, and frequency of meiotic recombination in the area b-vg second chromosome. It was found that the studied compounds - piridaben and proparhit have significant influence on vitality of D. melanogaster. The presence of these acaricides in the nutrition of flies testifies the harmful influence on their crossingover and reduced fecundity and longevity. We suggested to use the D. melanogaster as a test object for screening xenobiotics on acaricidal activity.

  12. Virtual Screening Techniques to Probe the Antimalarial Activity of some Traditionally Used Phytochemicals.

    Science.gov (United States)

    Shibi, Indira G; Aswathy, Lilly; Jisha, Radhakrishnan S; Masand, Vijay H; Gajbhiye, Jayant M

    2016-01-01

    Malaria parasites show resistance to most of the antimalarial drugs and hence developing antimalarials which can act on multitargets rather than a single target will be a promising strategy of drug design. Here we report a new approach by which virtual screening of 292 unique phytochemicals present in 72 traditionally important herbs is used for finding out inhibitors of plasmepsin-2 and falcipain-2 for antimalarial activity against P. falciparum. Initial screenings of the selected molecules by Random Forest algorithm model of Weka using the bioassay datasets AID 504850 and AID 2302 screened 120 out of the total 292 phytochemicals to be active against the targets. Toxtree scan cautioned 21 compounds to be either carcinogenic or mutagenic and were thus removed for further analysis. Out of the remaining 99 compounds, only 46 compounds offered drug-likeness as per the 'rule of five' criteria. Out of ten antimalarial drug targets, only two target proteins such as 3BPF and 3PNR of falcipain-2 and 1PFZ and 2BJU of plasmepsin-2 are selected as targets. The potential binding of the selected 46 compounds to the active sites of these four targets was analyzed using MOE software. The docked conformations and the interactions with the binding pocket residues of the target proteins were understood by 'Ligplot' analysis. It has been found that 8 compounds are dual inhibitors of falcipain-2 and plasmepsin-2, with the best binding energies. Compound 117 (6aR, 12aS)-12a-Hydroxy-9-methoxy-2,3-dimethylenedioxy-8-prenylrotenone (Usaratenoid C) present in the plant Millettia usaramensis showed maximum molecular docking score.

  13. 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....

  14. CORRELATION BETWEEN PHYTOCHEMICAL SCREENING, ANTIBACTERIAL AND ANTHELMINTIC ACTIVITIES OF ELAEOCARPUS SERRATUS

    Directory of Open Access Journals (Sweden)

    Kayal Sriti

    2011-09-01

    Full Text Available The petroleum ether, benzene, chloroform and acetone extracts of Elaeocarpus serratus were prepared by following Soxhlet method of extraction. Subsequently, phytochemical screening of the extracts was performed by following standard methods. While from the chloroform extract, alkaloids and anthraquinone glycosides were found, flavonoids and anthraquinone glycosides were present in the acetone extract. In addition, from petroleum ether extract, flavonoids were detected. On the other hand, anthraquinone glycosides were found in the benzene extract. None of the extracts showed any antibacterial and anthelmintic activities.

  15. Screening of Actinomycete Isolates from Niche Habitats in Manipur for Antibiotic Activity

    Directory of Open Access Journals (Sweden)

    Debananda S. Ningthoujam

    2009-01-01

    Full Text Available Problem statement: The exhaustion of the usual terrestrial sources and the rise of resistant pathogens dictate the search for novel actinomycetes and new antibiotics. In this context, niche habitats such as caves, pristine forests, lakes, rivers, and other wetlands, high salt environments, marine ecosystems and endophytic niches are promising targets for survey of bioactive actinomycetes. Approach: Actinomycetes were isolated from several niche habitats in Manipur, India, on selective media such as SCNA and Chitin agar with or without antibiotics. Selected isolates were subjected to antimicrobial activity screening by Kirby-Bauer method. Results: 172 lake sediment (SCNA, LS1 series, 35 lake sediment (CA, LSCH series, 120 river (NRP, NRB and..series, 39 forest (AML series, 35 cave (KC1 series, 101 salt spring (NH, N3S and .. series, 46 Shirui jungle (SJ series and 66 Shirui hill (SH series actinomycetes isolates were obtained. Of 99 randomly selected isolates screened, 37 had antimicrobial activities against 1 or more indicator strains: 32 against Gram positive bacteria and 8 against Gram negative bacteria; 10 actinomycete strains were antimycotic and 3 had broad-spectrum antibiotic activities. About 18 potent antibacterial, 1 anti pseudomonas, 1 exclusively antifungal and 3 broad-spectrum antimicrobial actinomycetes were chosen for further studies. Conclusion: Niche habitats in Manipur especially wetlands show great promise for discovery of bioactive actinomycetes.

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

    Science.gov (United States)

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

    2014-01-01

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

  17. Phytochemical Screening and Free-Radical Scavenging Activity of Bergenia stracheyi

    Directory of Open Access Journals (Sweden)

    Vinesh Kumar

    2013-07-01

    Full Text Available 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 glycosides. The free-radical scavenging activities of prepared extracts of Bergenia stracheyi were carried out using DPPH (1,1–Diphenyl-2-Picryl-Hydrazyl. The results of phytochemical screening of extracts confirmed the presence of amino acids, proteins, carbohydrates, glycosides, phenolics, steroids, and terpenoids in Bergenia stracheyi. The results showed that all extracts of Bergenia stracheyi had radical scavenging activity. The free-radical scavenging activities of Bergenia stracheyi extracts may be due to its polyphenol content. Further research should be carried out to isolates compounds with radical scavenging capacity for industrial applications.

  18. Anti-bacterial activities and phytochemical screening of extracts of different parts of Thalictrum rhynchocarpum.

    Science.gov (United States)

    Mayeku, Philip Wafula; Hassanali, Ahmed; Kiremire, Bernard Turyagenda; Odalo, Josiah Ochieng; Hertweck, Christian

    2013-01-01

    Parts of the plant Thalictrum rhyncocarpum are used in herbal medicine in Kenya to treat various infections. The aim of this study was to evaluate in-vitro anti-bacteria activities and phytochemical profiles of solvent extracts of the leaves, stem bark and root of Thalictrum rhyncocarpum against Bacillus subtilis-6633, Staphylococcus aures-SG 511, Escherichia coli SG 458, Pseudomonus aeruginosa-K799/61 and Mycobacterium vaccae-10670. 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 methanol root extract. Phytochemical screening of the extracts suggested the presence of glycosides and alkaloids in the stem bark and root extracts, and flavonoids and triterpenes in the leaf extracts. The study showed interesting levels of activities of solvent extracts of different parts of T. rhyncocarpum against some of the bacteria tested (M. vaccae, P. aeruginosa and B. subtilis). The results provide some scientific rationale for the traditional use of the plant in Kenya to treat different microbial infections.

  19. 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).

  20. 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

  1. Screening of plants used in Argentine folk medicine for antimicrobial activity.

    Science.gov (United States)

    Anesini, C; Perez, C

    1993-06-01

    Screening of 132 extracts from Argentine folk-medicinal plants for antimicrobial activity has been conducted using a penicillin G resistant strain of Staphylococcus aureus, Escherichia coli and Aspergillus niger as test microorganisms. Cephazolin, ampicillin and miconazole were used as standard antibiotics and concentration-response curves were obtained using the agar-well diffusion method. Boiling water extracts of plant materials were tested and 12 species were active against Staphylococcus aureus, whereas 10 were effective against Escherichia coli and 4 against Aspergillus niger. Tabebuia impetiginosa bark, Achyrocline sp. aerials parts, Larrea divaricata leaves, Rosa borboniana flowers, Punica granatum fruit pericarp, Psidium guineense fruit pericarp, Lithrea ternifolia leaves and Allium sativum bulbs produced some of the more active extracts.

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

    Directory of Open Access Journals (Sweden)

    Chuan-Ling Si

    2013-02-01

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

  3. Biological screening of some Turkish medicinal plant extracts for antimicrobial and toxicity activities.

    Science.gov (United States)

    Turker, A U; Usta, C

    2008-01-20

    Screening of antibacterial activity and toxicity of 22 aqueous plant extracts from 17 Turkish plants was conducted. Antibacterial activity was performed with six bacteria including Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Streptococcus pyogenes, Staphylococcus aureus and Staphylococcus epidermidis. Extracts of Tussilago farfara leaves, Helichyrsum plicatum flowers, Solanum dulcamara aerial parts and Urtica dioica leaves gave the best inhibitory activity against S. pyogenes, S. aureus and S. epidermidis. Of the 22 plant extracts, 20 extracts displayed toxicity (LC50 was radish seed bioassay, two different determinations (root length and seed germination) were performed with a comparison between two concentrations (50,000 mg L(-1) and 10,000 mg L(-1)). At low concentration (10,000 mg L(-1)), S. dulcamara aerial parts and Primula vulgaris leaf extracts were observed to inhibit the root length more than the other plant extracts. Also, the most inhibitive plant extract for seed germination was obtained with S. dulcamara aerial parts.

  4. 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.

  5. Are counterfeit or substandard anti-infective products the cause of treatment failure in Papua New Guinea?

    Science.gov (United States)

    Nair, Anita; Strauch, Stefanie; Lauwo, Jackson; Jähnke, Richard W O; Dressman, Jennifer

    2011-11-01

    Counterfeit and substandard products present a big challenge to any national plan or policy devised to improve public health. Poor quality drug products are especially a problem in lower income countries where product information and drug regulation enforcement are scant or absent. The primary aim of the present study was to evaluate the quality of amodiaquine and amoxicillin formulations sold in Papua New Guinea (PNG) and to detect the presence of counterfeit or substandard drugs in circulation, if any. Fourteen samples, collected from five registered pharmacies in Port Moresby, PNG, were subjected to visual inspection, quality control tests, and verification of product authenticity. The quality control tests included weight variation, content uniformity, thin layer chromatography, and dissolution. None of the products complied with all of the evaluation criteria. Two products, one of which was purportedly distributed by a company which proved to be nonexistent, contained no detectable amodiaquine. The present study confirms that counterfeit and substandard amodiaquine and amoxicillin products are finding their way into the distribution chain in Port Moresby, PNG. This quality problem with anti-infective products is of great concern, as it not only exposes patients to poor quality products but also fosters the development of resistant bacterial strains.

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

    Indian Academy of Sciences (India)

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

    2014-06-01

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

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

    Science.gov (United States)

    Hancock, Robert E W; Sahl, Hans-Georg

    2006-12-01

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

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

    Directory of Open Access Journals (Sweden)

    Natalie G Sanders

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

  9. Screening for and identification of starch-, amylopectin-, and pullulan-degrading activities in bifidobacterial strains.

    Science.gov (United States)

    Ryan, Sinéad M; Fitzgerald, Gerald F; van Sinderen, Douwe

    2006-08-01

    Forty-two bifidobacterial strains were screened for alpha-amylase and/or pullulanase activity by investigating their capacities to utilize starch, amylopectin, or pullulan. Of the 42 bifidobacterial strains tested, 19 were capable of degrading potato starch. Of these 19 strains, 11 were able to degrade starch and amylopectin, as well as pullulan. These 11 strains, which were shown to produce extracellular starch-degrading activities, included 5 strains of Bifidobacterium breve, 1 B. dentium strain, 1 B. infantis strain, 3 strains of B. pseudolongum, and 1 strain of B. thermophilum. Quantitative and qualitative enzyme activities were determined by measuring the concentrations of released reducing sugars and by high-performance thin-layer chromatography, respectively. These analyses confirmed both the inducible nature and the extracellular nature of the starch- and pullulan-degrading enzyme activities and showed that the five B. breve strains produced an activity that is consistent with type II pullulanase (amylopullulanase) activity, while the remaining six strains produced an activity with properties that resemble those of type III pullulan hydrolase.

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

    Directory of Open Access Journals (Sweden)

    Pushpendra Sharma

    2013-07-01

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

  11. 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...

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

    Directory of Open Access Journals (Sweden)

    Abha Shukla

    2015-01-01

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

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

    Science.gov (United States)

    Hawaze, S; Deti, H; Suleman, S

    2012-01-01

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

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

    Science.gov (United States)

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

    2015-01-01

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

  15. Using multiplexed regulation of luciferase activity and GFP translocation to screen for FOXO modulators

    Directory of Open Access Journals (Sweden)

    Carnero Amancio

    2009-02-01

    Full Text Available Abstract Background Independent luciferase reporter assays and fluorescent translocation assays have been successfully used in drug discovery for several molecular targets. We developed U2transLUC, an assay system in which luciferase and fluorescent read-outs can be multiplexed to provide a powerful cell-based high content screening method. Results The U2transLUC system is based on a stable cell line expressing a GFP-tagged FOXO transcription factor and a luciferase reporter gene under the control of human FOXO-responsive enhancers. The U2transLUC assay measures nuclear-cytoplasmic FOXO shuttling and FOXO-driven transcription, providing a means to analyze these two key features of FOXO regulation in the same experiment. We challenged the U2transLUC system with chemical probes with known biological activities and we were able to identify compounds with translocation and/or transactivation capacity. Conclusion Combining different biological read-outs in a single cell line offers significant advantages over conventional cell-based assays. The U2transLUC assay facilitates the maintenance and monitoring of homogeneous FOXO transcription factor expression and allows the reporter gene activity measured to be normalized with respect to cell viability. U2transLUC is suitable for high throughput screening and can identify small molecules that interfere with FOXO signaling at different levels.

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

    Directory of Open Access Journals (Sweden)

    Shimei eWu

    2016-02-01

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

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

    Science.gov (United States)

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

    2007-04-01

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

  18. 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.

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

    Science.gov (United States)

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

    2015-01-01

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

  20. 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

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

    Science.gov (United States)

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

    2016-01-01

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

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

    Science.gov (United States)

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

    1989-12-01

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

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

    Directory of Open Access Journals (Sweden)

    S S Patel

    2010-09-01

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

  4. Functional screening of hydrolytic activities reveals an extremely thermostable cellulase from a deep-sea archaeon

    Directory of Open Access Journals (Sweden)

    Benedikt eLeis

    2015-07-01

    Full Text Available Extreme habitats serve as a source of enzymes which are active under extreme conditions and are candidates for industrial applications. In this work, six large-insert mixed genomic libraries were screened for hydrolase activities in a broad temperature range (8 to 70 °C. Among a variety of hydrolytic activities, one fosmid clone, derived from a library of pooled isolates of hyperthermophilic archaea from deep sea vents, displayed hydrolytic activity on carboxymethyl cellulose substrate plates at 70 °C but not at lower temperatures. Sequence analysis of the fosmid insert revealed a gene encoding a novel glycoside hydrolase family 12 (GHF12 endo-1,4-β-glucanase, termed Cel12E. The enzyme shares 45 % sequence identity with a protein from the archaeon Thermococcus sp. AM4 and displays a unique multidomain architecture. Biochemical characterization of Cel12E revealed a remarkably thermostable protein, which appears to be of archaeal origin. The enzyme displayed maximum activity at 92 °C and was active on a variety of linear 1,4-β-glucans like carboxymethyl cellulose, β-glucan, lichenan, and phosphoric acid swollen cellulose. The protein is able to bind to various insoluble β-glucans. Product pattern analysis indicated that Cel12E is an endo-cleaving β-glucanase. Cel12E expands the toolbox of hyperthermostable archaeal cellulases with biotechnological potential.

  5. 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.

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

    OpenAIRE

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

    2016-01-01

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

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

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    Oliver N F King

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

  8. Survey of estrogenic activity in fish feed by yeast estrogen-screen assay.

    Science.gov (United States)

    Matsumoto, Takeru; Kobayashi, Makito; Moriwaki, Toshihisa; Kawai, Shin'ichiro; Watabe, Shugo

    2004-10-01

    Fishes have been used as laboratory animal for research of estrogenic endocrine disrupters by many researchers. However, much less attention was paid to the possibility that compounds with estrogenic activity are present in fish diets. In order to examine this possibility, we measured the estrogenic activity in commercial fish feed by in vitro yeast estrogen-screen (YES) assay based on the binding ability of tested compounds to estrogen receptors. Estrogenic activity was detected in all the commercial fish feed examined (0.2-6.2 ng estradiol equivalent/g fish feed), some phytoestrogens (genistein, formononetin, equol and coumestrol; relative activity to estradiol, 8.6 x 10(-6)-1.1 x 10(-4) by giving a value of 1.0 to estradiol) and some androgens (testosterone, 11-ketotestosterone and 5 alpha-dihydrotestosterone; relative activity to estradiol, 3.0 x 10(-6)-1.2 x 10(-4)). Therefore, it is possible that these compounds could affect the results of in vivo estrogen assay, such as vitellogenin production in male fish, especially when fish are fed commercial feed.

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

    Science.gov (United States)

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

    2005-05-13

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2013-01-01

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

  11. 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.

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

    Science.gov (United States)

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

    2014-01-01

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

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

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    Lydian Veldhuis

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2009-01-01

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

  15. Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries.

    Science.gov (United States)

    Minond, Dmitriy; Saldanha, S Adrian; Subramaniam, Prem; Spaargaren, Michael; Spicer, Timothy; Fotsing, Joseph R; Weide, Timo; Fokin, Valery V; Sharpless, K Barry; Galleni, Moreno; Bebrone, Carine; Lassaux, Patricia; Hodder, Peter

    2009-07-15

    VIM-2 is an Ambler class B metallo-beta-lactamase (MBL) capable of hydrolyzing a broad-spectrum of beta-lactam antibiotics. Although the discovery and development of MBL inhibitors continue to be an area of active research, an array of potent, small molecule inhibitors is yet to be fully characterized for VIM-2. In the presented research, a compound library screening approach was used to identify and characterize VIM-2 inhibitors from a library of pharmacologically active compounds as well as a focused 'click' chemistry library. The four most potent VIM-2 inhibitors resulting from a VIM-2 screen were characterized by kinetic studies in order to determine K(i) and mechanism of enzyme inhibition. As a result, two previously described pharmacologic agents, mitoxantrone (1,4-dihydroxy-5,8-bis([2-([2-hydroxyethyl]amino)ethyl]amino)-9,10-anthracenedione) and 4-chloromercuribenzoic acid (pCMB) were found to be active, the former as a non-competitive inhibitor (K(i)=K(i)(')=1.5+/-0.2microM) and the latter as a slowly reversible or irreversible inhibitor. Additionally, two novel sulfonyl-triazole analogs from the click library were identified as potent, competitive VIM-2 inhibitors: N-((4-((but-3-ynyloxy)methyl)-1H-1,2,3-triazol-5-yl)methyl)-4-iodobenzenesulfonamide (1, K(i)=0.41+/-0.03microM) and 4-iodo-N-((4-(methoxymethyl)-1H-1,2,3-triazol-5-yl)methyl)benzenesulfonamide (2, K(i)=1.4+/-0.10microM). Mitoxantrone and pCMB were also found to potentiate imipenem efficacy in MIC and synergy assays employing Escherichia coli. Taken together, all four compounds represent useful chemical probes to further investigate mechanisms of VIM-2 inhibition in biochemical and microbiology-based assays.

  16. 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

  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.

    Science.gov (United States)

    Mushtaq, Ahlam; Akbar, Seema; Zargar, Mohammad A; Wali, Adil F; Malik, Akhtar H; Dar, Mohammad Y; Hamid, Rabia; Ganai, Bashir A

    2014-01-01

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

    Science.gov (United States)

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

    2014-10-01

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

  19. 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.

  20. 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.

  1. 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.

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

    Directory of Open Access Journals (Sweden)

    Elizabeth Bilsland

    2016-01-01

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

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

    Directory of Open Access Journals (Sweden)

    C. Baskaran

    2011-06-01

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

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

    Science.gov (United States)

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

    2015-01-01

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

  5. Analysis of use of anti-infectives in the hospital pharmacy%某住院药房抗感染药物使用情况分析

    Institute of Scientific and Technical Information of China (English)

    李秀敏; 范胜军

    2010-01-01

    Objective To analyze the use of anti-infectives in our hospital pharmacy and to provide basis for rational clinical use of anti-infectives. Methods The analysis was conducted using the methods of defined daily use and order of consumption sum based on the raw data retrieved from Hospital Drug Inventory Management System. Results Anti-infectives using proportion after November droped. The use of varieties followed by the biggest amount of injection cefminox sodium,piperacillin sodium and sulbactam sodium for injection,cefazolin sodium needles. Medication is the highest frequency of piperacillin sodium and sulbactam sodium needles,cefminox needle,needle penicillin sodium. Conclusion Use of anti-infectives'situation wholely became stable. β-lactams,Quinolones was our clinical anti-infection treatment leading medicine. The individual frequency of use high variety took the amount rise,and it explained that still waited for the standard in antibiotics use.%目的 分析住院药房抗感染药物的使用情况,为临床合理应用抗感染药提供参考.方法 根据"药局库存管理程序"的原始数据资料,按金额、限定日剂量进行排序、分析.结果 抗感染药物使用比例从11月份后有所下降,使用金额最大的品种依次是注射用头孢米诺钠、注射用哌拉西林钠舒巴坦钠、头孢唑啉钠针,用药频率最高的是哌拉西林钠舒巴坦钠针、头孢米诺钠针、青霉素钠针.结论 抗感染用药情况整体趋稳,β-内酰胺类、喹诺酮类是临床抗感染治疗的主导药物,个别使用频率较高的品种占用金额上升,说明在抗菌药物的使用上仍有待规范.

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

    Science.gov (United States)

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

    2014-08-01

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

  7. 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…

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

    Science.gov (United States)

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

    2011-10-01

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

  9. Screening Antimicrobial Activity of Actinomycetes Isolated from Raja Ampat, West Papua, Indonesia

    Directory of Open Access Journals (Sweden)

    Wellyzar Sjamsuridzal

    2012-04-01

    Full Text Available In the framework of exploitation of antimicrobial activity of Actinomycetes in Papua, one hundred isolates ofActinomycetes isolated from soil and leaf litter samples from various ecosystems in Batanta and Salawati Island, RajaAmpat, West Papua were screened. We obtained 200 crude extracts from 100 isolates based on two extraction phases.Nonpolar metabolites were extracted by ethyl acetate : methanol (4:1 solvent while the polar metabolites wereconcentrated using a freeze-drying method. Based on the agar dilution method, a total of 43 from 200(21.5% crudeextracts have antimicrobial activity against bacteria and yeasts (Escherichia coli NBRC 14237, Bacillus subtilis NBRC3134, Staphylococcus aureus NBRC 13276, Micrococcus luteus NBRC 1367, Candida albicans NBRC 1594 andSaccharomyces cerevisiae NBRC 10217. Some crude extracts showed anti-Gram negative (1.5%, anti-Gram positive(17% and antifungal (17% activities. Crude metabolites which were extracted using ethyl acetate : methanol weremore effective on antimicrobial activity (35% compared with water extraction (17%. Five most potential isolates (BL-13-5, BL-06-5, BL-14-2, BL-22-3, and Sl-36-1 were identified based on 16S rRNA gene sequence data. Sequencesimilarity search by BLAST program revealed that they show sequence similarities to Streptomyces kanamyceticus(92%, Streptomyces verne (92%, Streptomyces narbonensis (92%, Streptomyces malachitofuscus (98%, andStreptomyces hygroscopicus (96%, respectively.

  10. 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.

  11. 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.

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

    Directory of Open Access Journals (Sweden)

    Ali M El-Halawany

    2011-01-01

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

  13. Phytochemical screening, antiglycation and antioxidant activities of whole plant of Boerhavia repens L. from Cholistan, Pakistan.

    Science.gov (United States)

    Nazneen, Fariha; Sheikh, Munir A; Jameel, Amir; Rahman, Ziaur

    2016-05-01

    Present study was aimed to explore a traditionally used indigenous medicinal plant Boerhavia repens (Nyctaginaceae family) of the Cholistan desert, Pakistan. Crude aqueous and methanolic extracts of the whole plant were investigated in vitro for preliminary phytochemical screening, antioxidant and antiglycation activities. Antioxidant activities were determined by total phenolic contents, 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging and inhibition of lipid peroxidation. For antiglycation activities browning production was noted and thiobarbituric acid (TBA) technique was used to determine glycation level. Boerhavia repens expressed considerable amounts of phytochemicals. Extract yield was found to be 4.59%-7.85% g/100g of dry matter with total phenolics ranging from 47.9- 190.77mg/GAE per g for aqueous and methanol extract respectively. Strong inhibitory effect was exhibited by methanolic extract in linoleic acid per oxidation system (86.11%, EC50=0.99mg/mL) and DPPH assay (88.65%, EC50=212.33μg/ml). In term of browning maximum inhibition (81.50%) was exhibited by methanolic extract at 37°C at third week of incubation. Both extracts expressed significant (P>0.05) and comparable inhibition of glycation level. In conclusion, Boerhavia repens showed promising antioxidant and antiglycation activities validating its therapeutic potential.

  14. Pharmacognostic Screening, Phytochemical Evaluation and In- Vitro free radical Scavenging Activity of Acacia leucophloea Root

    Institute of Scientific and Technical Information of China (English)

    Deenanath Jhade; Sachin Jain; Ankit Jain; Praveen Sharma

    2012-01-01

    Objective: Pharmacognostic Screening and evaluate the in-vitro free radical scavenging activity of roots Acacia leucophloea. Methods: Pharmacognostic Standardization, Physico-chemical evaluation of the roots of Acacia leucophloea was carried out to determine its macro-and microscopical characters and also some of its quantitative standards. Microscopical studies were done by using trinocular microscope. Microscopically, root showed cork, cortex, stellar region and calcium oxalate crystals. Petroleum ether, ethanol, aqueous extracts of Acacia leucophloea were prepared, with successive extraction in soxhlet apparatus. Each extract was selected to study the free radical scavenging activity by superoxide scavenging assay method. Results: It was found that aqueous extract contained carbohydrates, glycosides amino acids flavonoids, tannins, alkaloids, steroids; ethanolic extract contained glycosides amino acids flavonoids, tannins, alkaloids, steroids. Ethanolic extract of Acacia leucophloea shows maximam inhibition in superoxide scavenging model. Aqueous extract also showed almost similar activity compared to ethanolic extract), while Petroleum ether extract showed poor inhibition of superoxide scavenging activity. Conclusion: The present study on pharmacognostic standardization, physico and phytochemical evaluation of Acacia leucophloea root might be useful to supplement information about its identification parameters assumed significantly in the way of acceptability of herbal drugs in present scenario lacking regulatory laws to control quality of herbal drugs.

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

    Science.gov (United States)

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

    2000-06-01

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

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

    Science.gov (United States)

    McCullough, Cheryl E.; Marmorstein, Ronen

    2016-01-01

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

  17. 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.

  18. Function-Based Metagenomic Library Screening and Heterologous Expression Strategy for Genes Encoding Phosphatase Activity.

    Science.gov (United States)

    Villamizar, Genis A Castillo; Nacke, Heiko; Daniel, Rolf

    2017-01-01

    The release of phosphate from inorganic and organic phosphorus compounds can be mediated enzymatically. Phosphate-releasing enzymes, comprising acid and alkaline phosphatases, are recognized as useful biocatalysts in applications such as plant and animal nutrition, bioremediation and diagnostic analysis. Metagenomic approaches provide access to novel phosphatase-encoding genes. Here, we describe a function-based screening approach for rapid identification of genes conferring phosphatase activity from small-insert and large-insert metagenomic libraries derived from various environments. This approach bears the potential for discovery of entirely novel phosphatase families or subfamilies and members of known enzyme classes hydrolyzing phosphomonoester bonds such as phytases. In addition, we provide a strategy for efficient heterologous phosphatase gene expression.

  19. Screening bioactives reveals nanchangmycin as a broad spectrum antiviral active against Zika virus

    Science.gov (United States)

    Rausch, Keiko; Hackett, Brent; Weinbren, Nathan; Reeder, Sophia; Sadovsky, Yoel; Hunter, Christopher; Schultz, David C.; Coyne, Carolyn; Cherry, Sara

    2017-01-01

    Zika virus is an emerging arthropod-borne flavivirus for which there are no vaccines or specific therapeutics. We screened a library of 2000 ‘bioactive’ compounds for their ability to block Zika virus infection in three distinct cell-types with two different strains of Zika virus. Using a microscopy-based assay, we validated 38 drugs that inhibited Zika virus infection, including FDA approved nucleoside analogs. Cells expressing high levels of the attachment factor AXL can be protected from infection with receptor tyrosine kinase inhibitors, while placental-derived cells that lack AXL expression are insensitive to this inhibition. Importantly, we identified nanchangmycin as a potent inhibitor of Zika virus entry across all cell types tested including physiologically relevant primary cells. Nanchanmycin was also active against other medically relevant viruses including West Nile, dengue, and chikungunya virus that use a similar route of entry. This study provides a resource of small molecules to study Zika virus pathogenesis. PMID:28099856

  20. Local community intervention through depression screening and group activity for elderly suicide prevention.

    Science.gov (United States)

    Oyama, Hirofumi; Ono, Yutaka; Watanabe, Naoki; Tanaka, Eriko; Kudoh, Seijiro; Sakashita, Tomoe; Sakamoto, Shinji; Neichi, Keiko; Satoh, Kyoko; Nakamura, Kenji; Yoshimura, Kimio

    2006-02-01

    This study aims to evaluate outcomes of a community-based program to prevent suicide among the elderly (>or=65 years old) using a quasi-experimental design with two neighboring references. During 1999-2004, the program including depression screening and group activity was conducted by the public health nurses in the Minami district (population 1685) of Nagawa town, rural Japan. Pre-post changes in the risk of completing suicide were estimated by the incidence rate ratios (IRR). The risk for Minami's elderly females was reduced by 74% (age-adjusted IRR, 0.26; 90% CI, 0.07-0.98) more than the historical trend, while there was no change in the risk of Minami's males and nor in the male or female references. The local intervention using public health nursing would be effective against suicide for elderly females without diffusing to the surroundings.

  1. Material screening metrics and optimal performance of an active magnetic regenerator

    Science.gov (United States)

    Niknia, I.; Trevizoli, P. V.; Christiaanse, T. V.; Govindappa, P.; Teyber, R.; Rowe, A.

    2017-02-01

    A variety of metrics to rank the magnetocaloric materials can be found in the literature, but a quantitative assessment showing their efficacy has not been reported. A numerical model of an active magnetic regenerator cycle is used to assess the predictive ability of a set of material metrics. The performance of eight cases of known magnetocaloric material (including first order MnFeP1-xAsx and second order materials Gd, GdDy, Tb), and 15 cases of hypothetical materials are considered. Using a fixed regenerator matrix geometry, magnetic field, and flow waveforms, the maximum exergetic cooling power of each material is identified. Several material screening metrics such as relative cooling power (RCP) are tested and a linear correlation is found between maximum RCP and the maximum exergetic cooling power. The sensitivity of performance to variations in the hot side and cold side temperatures from the conditions giving maximum exergetic power are determined.

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

    Directory of Open Access Journals (Sweden)

    Deepak.TK

    2014-08-01

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

  3. 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.

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

    Directory of Open Access Journals (Sweden)

    H.M. Inuwa

    2012-02-01

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

  5. 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.

  6. 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

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

    Directory of Open Access Journals (Sweden)

    Hideki Hayashi

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

  8. Sensitive fluorimetric assays for α-glucosidase activity and inhibitor screening based on β-cyclodextrin-coated quantum dots.

    Science.gov (United States)

    Liu, Si-Yao; Wang, Huan; He, Tian; Qi, Liang; Zhang, Zhi-Qi

    2016-02-01

    A fluorescence method was established for a α-glucosidase activity assay and inhibitor screening based on β-cyclodextrin-coated quantum dots. p-Nitrophenol, the hydrolysis product of the α-glucosidase reaction, could quench the fluorescence of β-cyclodextrin-coated quantum dots via an electron transfer process, leading to fluorescence turn-off, whereas the fluorescence of the system turned on in the presence of α-glucosidase inhibitors. Taking advantage of the excellent properties of quantum dots, this method provided a very simple, rapid and sensitive screening method for α-glucosidase inhibitors. Two α-glucosidase inhibitors, 2,4,6-tribromophenol and acarbose, were used to evaluate the feasibility of this screening model, and IC50 values of 24 μM and 0.55 mM were obtained respectively, which were lower than those previously reported. The method may have potential application in screening α-glucosidase inhibitors.

  9. Investigation of plasma parameters in an active screen cage-pulsed dc plasma used for plasma nitriding

    Science.gov (United States)

    Naeem, M.; Khattak, Z. I.; Zaka-ul-Islam, M.; Shabir, S.; Khan, A. W.; Zakaullah, M.

    2014-11-01

    Active screen cage-pulsed dc plasmas are widely used in the material processing applications such as plasma nitriding, carburizing and nitrocarburizing. Specifically for plasma nitriding applications, a H2-N2 mixture is used. In this article, a study of the electron number density (ne), atomic nitrogen density ([N]), electron temperature ? and the excitation temperature ? is reported in the presence of an active screen cage-pulsed dc plasma. The ne and ? are determined here by a triple Langmuir probe, while [N] and ? are estimated by optical emission spectroscopy (OES). The two temperatures and their ratio ? are compared for different input parameters (such as applied power, gas pressure and H2 percentage). This study is useful in active screen cage plasma nitriding applications where only few plasma diagnostic measurements have been reported.

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

    Directory of Open Access Journals (Sweden)

    A.S.N. Formagio

    2015-04-01

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

  11. Screening of actinomycetes from earthworm castings for their antimicrobial activity and industrial enzymes

    Directory of Open Access Journals (Sweden)

    Vijay Kumar

    2012-03-01

    Full Text Available Actinomycetes from earthworm castings were isolated and screened for their antimicrobial activity and industrial enzymes. A total of 48 isolates were obtained from 12 samples of earthworm castings. Highest numbers of isolates were recovered from forest site (58.33 % as compared to grassland (25% and agricultural land (16.66%. The growth patterns, mycelial coloration of abundance actinomycetes were documented. The dominant genera Identified by cultural, morphological and physiological characteristics were Streptomyces (60.41% followed by Streptosporangium (10.41%, Saccharopolyspora (6.25% and Nocardia (6.25%. Besides these, other genera like Micromonospora, Actinomadura, Microbispora, Planobispora and Nocardiopsis were also recovered but in low frequency. Among the 48 isolates, 52.08% were found active against one or more test organisms. Out of 25 active isolates 16% showed activity against bacterial, human fungal as well as phytopathogens. Among 48 isolates 38, 32, 21, 20, 16 and 14 produced enzyme amylase, caseinase, cellulase, gelatinase, xylanase and lipase respectively while 10 isolates produced all the enzymes. More interestingly 2, 3, and 1 isolates produced amylase, xylanase and lipase at 45°C respectively. In the view of its antimicrobial activity as well as enzyme production capability the genus Streptomyces was dominant. The isolate EWC 7(2 was most promising on the basis of its interesting antimicrobial activity and was identified as Streptomyces rochei. The results of these findings have increased the scope of finding industrially important actinomycetes from earthworm castings and these organisms could be promising sources for industrially important molecules or enzymes.

  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. 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.

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

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    Sara Pereira

    2015-06-01

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

  15. RNAi screen identifies Jarid1b as a major regulator of mouse HSC activity

    Science.gov (United States)

    Cellot, Sonia; Hope, Kristin J.; Chagraoui, Jalila; Sauvageau, Martin; Deneault, Éric; MacRae, Tara; Mayotte, Nadine; Wilhelm, Brian T.; Landry, Josette R.; Ting, Stephen B.; Krosl, Jana; Humphries, Keith; Thompson, Alexander; Sauvageau, Guy

    2017-01-01

    Histone methylation is a dynamic and reversible process proposed to directly impact on stem cell fate. The Jumonji (JmjC) domain–containing family of demethylases comprises 27 members that target mono-, di-, and trimethylated lysine residues of histone (or nonhistone) proteins. To evaluate their role in regulation of hematopoietic stem cell (HSC) behavior, we performed an in vivo RNAi-based functional screen and demonstrated that Jarid1b and Jhdm1f play opposing roles in regulation of HSC activity. Decrease in Jarid1b levels correlated with an in vitro expansion of HSCs with preserved long-term in vivo lymphomyeloid differentiation potential. Through RNA sequencing analysis, Jarid1b knockdown was associated with increased expression levels of several HSC regulators (Hoxa7, Hoxa9, Hoxa10, Hes1, Gata2) and reduced levels of differentiation-associated genes. shRNA against Jhdmlf, in contrast, impaired hematopoietic reconstitution of bone marrow cells. Together, our studies identified Jarid1b as a negative regulator of HSC activity and Jhdmlf as a positive regulator of HSC activity. PMID:23777767

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

    Science.gov (United States)

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

    2008-01-01

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

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

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    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.

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

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    Maharaj Rajendra

    2012-09-01

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

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

    Science.gov (United States)

    Hamada, Nagwa Mohamed Mahrous; Abdo, Nadia Yousef Megally

    2015-06-08

    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. 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.

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

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    Mohammed A. Alshawsh

    2009-01-01

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

  2. 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.

  3. Profiling physical activity, diet, screen and sleep habits in Portuguese children.

    Science.gov (United States)

    Pereira, Sara; Katzmarzyk, Peter T; Gomes, Thayse Natacha; Borges, Alessandra; Santos, Daniel; Souza, Michele; dos Santos, Fernanda K; Chaves, Raquel N; Champagne, Catherine M; Barreira, Tiago V; Maia, José A R

    2015-06-02

    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).

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

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    Ranveer Singh Jayani

    2010-01-01

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

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

    Science.gov (United States)

    Pereira, Sara; Katzmarzyk, Peter T.; Gomes, Thayse Natacha; Borges, Alessandra; Santos, Daniel; Souza, Michele; dos Santos, Fernanda K.; Chaves, Raquel N.; Champagne, Catherine M.; Barreira, Tiago V.; Maia, José A.R.

    2015-01-01

    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). PMID:26043034

  6. PHYTOCHEMICAL SCREENING AND ANTHELMINTIC ACTIVITY STUDY OF SARACA INDICA LEAVES EXTRACTS

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    Nayak Sarojini

    2011-05-01

    Full Text Available To know the anthelmintic property of leaves of Saraca indica, we used both maceration and soxhelet methods of extraction using solvents like ethanol and methanol. Each extract was tested for its anthelmintic activity by following standard method. The ethanolic and methanolic extracts (obtained from both the methods of extractions of Saraca indica displayed anthelmintic property in a dose-dependant manner. In both the methods of extraction, we found that the ethanolic as well as the methanolic extracts were more potent than the positive control as far as anthelminthic property was concerned. To correlate phytochemical screening with anthelmintic activity, phytochemical evaluation of the extracts was also performed. From our result, it may be mentioned that the ethanolic extract was relatively more potent as an anthelmintic agent due to the presence of alkaloids, glycosides, tannins and flavonoids. On the other hand, the methanolic extract was effective as an anthelmintic agent probably due to the involvement of glycosides and flavonoids. The presence of alkaloids, glycosides, terpenoids, tannins and flavonoids seems to be the responsible phytochemical constituents for demonstrating anthelmintic activities of our extracts.

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

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    Selvameenal L

    2009-01-01

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

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

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    Xian-Ying Yang

    2016-08-01

    Full Text Available Objective: 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.

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

    Science.gov (United States)

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

    2016-01-01

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2013-01-01

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2013-01-01

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

  12. 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.

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

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    Vijay Kumar

    2013-09-01

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

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

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    Shweta S Saboo

    2014-01-01

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

  15. 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.

  16. Development and Validation of a High Throughput Screen for Compounds with Antiviral Activity Against Encephalitic Alphaviruses

    Science.gov (United States)

    2010-09-15

    determined the compounds as cytotoxic if the viability is less than 85% in the screening. 1. Single dose study A. Small library screening We have...run on two independent days and the results are shown below (Table 8). The assay metrics meet the requirement for a successful HTS assay for a library ... screening . The assay performance was ascertained by testing plate-to-plate variation (data not shown). Table 8. Assay performance of the assay

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

    Science.gov (United States)

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

    2014-08-01

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

  18. Microplate assay for screening the antibacterial activity of Schiff bases derived from substituted benzopyran-4-one.

    Science.gov (United States)

    Amin, Rehab M; Abdel-Kader, Nora S; El-Ansary, Aida L

    2012-09-01

    Schiff bases (SB(1)-SB(3)) were synthesized from the condensation of 6-formyl-7-hydroxy-5-methoxy-2-methylbenzopyran-4-one with 2-aminopyridine (SB(1)), p-phenylenediamine (SB(2)) and o-phenylenediamine (SB(3)), while Schiff bases (SB(4)-SB(6)) were synthesized by condensation of 5,7-dihydroxy-6-formyl-2-methylbenzopyran-4-one with 2-aminopyridine (SB(4)), p-phenylenediamine (SB(5)) and o-phenylenediamine (SB(6)). Schiff bases were characterized using elemental analysis, IR, UV-Vis, (1)H NMR, (13)C NMR and mass spectroscopy. These compounds were screened for antibacterial activities by micro-plate assay technique. Escherichia coli and Staphylococcus capitis were exposed to different concentrations of the Schiff bases. Results showed that the antibacterial effect of these Schiff bases on Gram-negative bacteria were higher than that on Gram-positive bacteria moreover, the Schiff bases containing substituent OCH(3) on position five have higher antibacterial activity than that containing hydroxy group on the same position.

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

    Directory of Open Access Journals (Sweden)

    Milena Nikolova

    2011-01-01

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

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

    Science.gov (United States)

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

    2016-01-01

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

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

    Directory of Open Access Journals (Sweden)

    Udaysing Hari Patil,

    2011-01-01

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

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

    Science.gov (United States)

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

    2016-01-01

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

  3. 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

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

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    Sanchez Nelson F

    2012-06-01

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

  5. Phytochemical screening, acute toxicity, anxiolytic and antidepressant activities of the Nelumbo nucifera fruit.

    Science.gov (United States)

    Rajput, Muhammad Ali; Khan, Rafeeq Alam

    2017-02-01

    Recently use of herbal therapies and diet rich in flavonoids and vitamin C have increased significantly to treat minor to modest anxiety disorders and various forms of depression. But further research and studies are necessary to evaluate the pharmacological & toxicological effects of plants. Hence present study was designed to conduct phytochemical screening, acute toxicity study, anxiolytic and antidepressant activities of the ethanol extract of Nelumbo nucifera fruit in order to ascertain its therapeutic potential. The qualitative phytochemical screening of the seed pods of the N. nucifera fruit extract exposed the existence of flavonoids, saponins, alkaloids, tannins and terpenoids in it. The acute toxicity of the N. nucifera fruit extract in mice revealed its LD50 value to be greater than 5000 mg/kg. Antianxiety activity was determined by elevated plus maze and light and dark test using 35 male Wister rats weighing 200-220 g which were equally divided in to 5 groups. The animals used in EPM underwent testing in light and dark box just 30 min after EPM. The antidepressant effect was assessed by forced swimming test using 35 male albino mice weighing 20-25 g equally divided in to 5 groups. In elevated plus maze, N. nucifera fruit extract exhibited substantial rise in number of open arm entries and time spent in open arms at dose 50 mg/kg while highly noteworthy increase in both parameters were observed at extract doses 100 and 200 mg/kg as compared to control. In light dark test highly significant increase in the percentage of time spent in light compartment was observed as compared to control. In forced swimming test highly noteworthy decline in duration of immobility was recorded at doses 100 and 200 mg/kg on 15th day i-e after administration of 14 doses, as compared to control; whereas same doses demonstrated significant decrease as compared to control in duration of immobility after single dose administration i-e on 2nd day of experiment. Thus N

  6. 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

    2015-01-01

    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 colle

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

    Institute of Scientific and Technical Information of China (English)

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

    2008-01-01

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

  8. Validity of “sputtering and re-condensation” model in active screen cage plasma nitriding process

    Energy Technology Data Exchange (ETDEWEB)

    Saeed, A., E-mail: phyadi@gmail.com [Department of Physics, Gomal University, 29050 D.I. Khan (Pakistan); National Centre for Physics, Quaid-i-Azam University Campus Islamabad 45320 (Pakistan); Khan, A.W. [Department of Physics, Gomal University, 29050 D.I. Khan (Pakistan); National Centre for Physics, Quaid-i-Azam University Campus Islamabad 45320 (Pakistan); Jan, F. [Department of Physics, Quaid-i-Azam University, 45320 Islamabad (Pakistan); Abrar, M. [Institute of Physics and Electronics, University of Peshawar, 25120 Peshawar (Pakistan); Khalid, M. [Department of Physics, Gomal University, 29050 D.I. Khan (Pakistan); Zakaullah, M. [Department of Physics, Quaid-i-Azam University, 45320 Islamabad (Pakistan)

    2013-05-15

    The validity of “sputtering and re-condensation” model in active screen plasma nitriding for nitrogen mass transfer mechanism is investigated. The dominant species including NH, Fe-I, N{sub 2}{sup +}, N-I and N{sub 2} along with H{sub α} and H{sub β} lines are observed in the optical emission spectroscopy (OES) analysis. Active screen cage and dc plasma nitriding of AISI 316 stainless steel as function of treatment time is also investigated. The structure and phases composition of the nitrided layer is studied by X-ray diffraction (XRD). Surface morphology is studied by scanning electron microscopy (SEM) and hardness profile is obtained by Vicker's microhardness tester. Increasing trend in microhardness is observed in both cases but the increase in active screen plasma nitriding is about 3 times greater than that achieved by dc plasma nitriding. On the basis of metallurgical and OES observations the use of “sputtering and re-condensation” model in active screen plasma nitriding is tested.

  9. T & I--Graphic Arts, Silk Screen Printing. Kit No. 60. Instructor's Manual [and] Student Learning Activity Guide.

    Science.gov (United States)

    Cope, George

    An instructor's manual and student activity guide on silk screen printing are provided in this set of prevocational education materials which focuses on the vocational area of trade and industry (graphic arts). (This set of materials is one of ninety-two prevocational sets arranged around a cluster of seven vocational offerings: agriculture, home…

  10. Screening for proteolytic activities in snake venom by means of a multiplexing electrospray ionization mass spectrometry assay scheme

    NARCIS (Netherlands)

    Liesener, André; Perchuc, Anna-Maria; Schöni, Reto; Wilmer, Marianne; Karst, Uwe

    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 characteriza

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

    Directory of Open Access Journals (Sweden)

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

    Directory of Open Access Journals (Sweden)

    Riaz Tauheeda

    2012-01-01

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

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

    Institute of Scientific and Technical Information of China (English)

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

    2014-01-01

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

  14. Establishment of a transgenic yeast screening system for estrogenicity and identification of the anti-estrogenic activity of malachite green.

    Science.gov (United States)

    Jiao, Baowei; Yeung, Eric K C; Chan, Chi Bun; Cheng, Christopher H K

    2008-12-15

    Endocrine disruptors refer to chemical compounds in the environment which interfere with the endocrine systems of organisms. Among them, environmental estrogens pose serious problems to aquatic organisms, in particular fish. It is therefore important and necessary to have a fast and low-cost system to screen the large number of different chemical compounds in the aquatic environment for their potential endocrine disrupting actions. In this study, a screening platform was developed to detect xenoestrogens in the aquatic environment using the fission yeast Schizosaccharomyces pombe, and applied for compound screening. The aim was to demonstrate any significant potential differences between the fish screening system and the human screening system. To this end, a yeast expression vector harboring a fish estrogen receptor alpha and a reporter vector containing the estrogen responsive element fused with the Escherichia coli LacZ gene were constructed. After transformation with these two vectors, the transformed yeast clones were confirmed by Western blotting and selected on the basis of the beta-galactosidase activity. In this transgenic yeast system, the natural estrogen (estradiol) and other known xenoestrogens such as diethylstilbestrol, bisphenol A, genistein and dichloro-diphenyl-trichloroethane exhibited dose-dependent activities. Using this system, more than 40 putative endocrine disruptors including phytoestrogens, pesticides, herbicides, industrial dyes and other industrial chemicals were screened. Ten of them were demonstrated to exhibit estrogenic actions. Industrial dyes such as malachite green (MG) that disrupt thyroid hormone synthesis are extensively used and are widely distributed in the aquatic environment. Using this system, MG did not show any estrogenic action, but was demonstrated to exhibit anti-estrogenic activity.

  15. 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.

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

    Institute of Scientific and Technical Information of China (English)

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

    2014-01-01

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

  17. 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.

  18. 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.

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

    Directory of Open Access Journals (Sweden)

    Junaid Iqbal

    2013-01-01

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

  20. Label-free, turn-on fluorescent sensor for trypsin activity assay and inhibitor screening.

    Science.gov (United States)

    Zhang, Lufeng; Qin, Haiyan; Cui, Wanwan; Zhou, Yang; Du, Jianxiu

    2016-12-01

    The development of new detection methods for proteases activity assay is important in clinical diagnostics and drug development. In this work, a simple, label-free, and turn-on fluorescent sensor was fabricated for trypsin, a protease produced in the pancreas. Cytochrome c, a natural substance of trypsin, could be selectively cleaved by trypsin into heme-peptide fragment. The produced heme-peptide fragment exhibited an intensive catalytic role on the H2O2-mediated the oxidation of thiamine to form strong fluorescent thiochrome. The fluorescence intensity was closely dependent on the amount of trypsin presented. The procedure allowed the measurement of trypsin over the range of 0.5-20.0μg/mL with a detection limit of 0.125μg/mL. The sensor showed better precision with a relative standard deviation of 1.6% for the measurement of 1.0μg/mL trypsin solution (n=11). This sensing system was applied to screen the inhibitor of trypsin, the IC50 values were calculated to be 12.71ng/mL for the trypsin inhibitor from soybean and 2.0μg/mL for benzamidine hydrochloride, respectively, demonstrating its potential application in drug development and related diseases treatment.

  1. 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.

  2. Screening of catalytic oxygen reduction reaction activity of metal-doped graphene by density functional theory

    Energy Technology Data Exchange (ETDEWEB)

    Chen, Xin, E-mail: chenxin830107@pku.edu.cn; Chen, Shuangjing; Wang, Jinyu

    2016-08-30

    Highlights: • The screened M-G structures are very thermodynamically stable, and the stability is even higher than that of the corresponding bulk metal surfaces. • The binding energies of ORR intermediates suggest that they are not linear dependence, which are different form the cases found on some metal-based catalysts. • The Au-, Co-, and Ag-G structures could be used as the ORR catalysts. - Abstract: Graphene doping is a promising direction for developing effective oxygen reduction reaction (ORR) catalysts. In this paper, we computationally investigated the ORR performance of 10 kinds of metal-doped graphene (M-G) catalysts, namely, Al-, Si-, Mn-, Fe-, Co-, Ni-, Pd-, Ag-, Pt-, and Au-G. The results shown that the binding energies of the metal atoms incorporated into the graphene vacancy are higher than their bulk cohesive energies, indicating the formed M-G catalysts are even more stable than the corresponding bulk metal surfaces, and thus avoid the metals dissolution in the reaction environment. We demonstrated that the linear relation among the binding energies of the ORR intermediates that found on metal-based materials does not hold for the M-G catalysts, therefore a single binding energy of intermediate alone is not sufficient to evaluate the ORR activity of an arbitrary catalyst. By analysis of the detailed ORR processes, we predicted that the Au-, Co-, and Ag-G materials can be used as the ORR catalysts.

  3. Virtual Screening of compounds from Tabernaemontana divaricata for potential anti-bacterial activity

    Science.gov (United States)

    Gogoi, Rashmi Rekha; Gogoi, Dhrubajyoti; Bezbaruah, Rajib Lochan

    2014-01-01

    Virtual Screening and Molecular Docking analysis for Tabernaemontana divaricata derived 66 Law Molecular Weight Compounds (LMW) was conducted and to identified and predicted novel molecules as a inhibitor of Streptococcus pneumonia. The investigation has revealed several compounds with optimum binding towards Penicillin-binding proteins, Sialidases, Aspartate betasemialdehide dehydrogenase cell membrane protein of Streptococcus pneumonia. Docking results were computed in term of binding energy, ligand efficiency and number of hydrogen bonding. Apparicine (-5.14), 5-Hydroxyvoaphylline (-4.78), Voacangine (-4.7), 19-Hydroxycoronaridine (-4.44) and Coronaridine (-4.72) are identified as most suitable to bind with N-acetylglucosamine-1- phosphate uridyltransferase receptor. Ervaticine (-6.33), Ibogamine (-6.15), Methylvoaphylline (-5.74) and Coronaridine hydroxyindolenine (-5.32) has showed novel binding against the penicillin-binding proteins. Ervaticine (-6.42), 5-oxo-11-hydroxy voaphylline (-6.18), Conolobine B (-6.02) has found optimum binding against the active site of NanB sialidase of Streptococcus pneumonia. The compounds 3S-Cyanocoronaridine (-6.71), 19-Epivoacristine (-5.48) and Ervaticine(-5.45) interacting with aspartate beta-semialdehide and found suitable with least docking score. PMID:24748755

  4. Immobilized magnetic beads-based multi-target affinity selection coupled with HPLC-MS for screening active compounds from traditional Chinese medicine and natural products.

    Science.gov (United States)

    Chen, Yaqi; Chen, Zhui; Wang, Yi

    2015-01-01

    Screening and identifying active compounds from traditional Chinese medicine (TCM) and other natural products plays an important role in drug discovery. Here, we describe a magnetic beads-based multi-target affinity selection-mass spectrometry approach for screening bioactive compounds from natural products. Key steps and parameters including activation of magnetic beads, enzyme/protein immobilization, characterization of functional magnetic beads, screening and identifying active compounds from a complex mixture by LC/MS, are illustrated. The proposed approach is rapid and efficient in screening and identification of bioactive compounds from complex natural products.

  5. 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.

  6. 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.

  7. Development and Application of a High-Throughput Screening Method to Evaluate Antifungal Activity against Trichophyton tonsurans.

    Science.gov (United States)

    Preuett, Barry; Leeder, J Steven; Abdel-Rahman, Susan

    2015-10-01

    There exist relatively few drug classes on the market to treat dermatophyte infections. This investigation was designed to develop and validate high-throughput methodology for screening and confirmation of chemicals for activity against Trichophyton tonsurans. Growth characteristics were examined on two platforms (96- and 384-well) in three media at eight spore concentrations over a period of up to 120 h. Microspectrophotometry was used to automate plate reads. The 384-well platform was used to screen more than 7000 compounds from six chemical libraries. Z-scores for optical density relative to positive growth controls were used to flag compounds of interest and activity confirmed in separate assays. The final conditions selected for both screening and confirmation with minimum inhibitory concentration (MIC) determination were growth for 48 h at 32 °C in SabDex with 1 × 10(4) spores per reaction. Sensitivity and specificity averaged 99.2% (range, 95.2%-100%) and 99.8% (range, 99.1%-100%), respectively. MICs for known antifungals were similar to those reported by others using Clinical and Laboratory Standards Institute methods. Several novel compound classes were identified to have activity against T. tonsurans with potency comparable to known antifungals. A robust, reproducible assay is described that permits high-throughput screening in T. tonsurans.

  8. Simulated Screens of DNA Encoded Libraries: The Potential Influence of Chemical Synthesis Fidelity on Interpretation of Structure-Activity Relationships.

    Science.gov (United States)

    Satz, Alexander L

    2016-07-11

    Simulated screening of DNA encoded libraries indicates that the presence of truncated byproducts complicates the relationship between library member enrichment and equilibrium association constant (these truncates result from incomplete chemical reactions during library synthesis). Further, simulations indicate that some patterns observed in reported experimental data may result from the presence of truncated byproducts in the library mixture and not structure-activity relationships. Potential experimental methods of minimizing the presence of truncates are assessed via simulation; the relationship between enrichment and equilibrium association constant for libraries of differing purities is investigated. Data aggregation techniques are demonstrated that allow for more accurate analysis of screening results, in particular when the screened library contains significant quantities of truncates.

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

    Directory of Open Access Journals (Sweden)

    Okoh Anthony I

    2010-05-01

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

  10. Screening for alternative antibiotics: an investigation into the antimicrobial activities of medicinal food plants of Mauritius.

    Science.gov (United States)

    Mahomoodally, M F; Gurib-Fakim, A; Subratty, A H

    2010-04-01

    The present study was designed to evaluate the antimicrobial activities of 2 endemic medicinal plants; Faujasiopsis flexuosa (Asteraceae) (FF) and Pittosporum senacia (Pittosporaceae) (PS) and 2 exotic medicinal plants, Momordica charantia (Cucurbitaceae) (MC) and Ocimum tenuiflorum (Lamiaceae) (OT) that forms part of local pharmacopoeia of Mauritius and correlate any observed activity with its phytochemical profile. Aqueous and organic fractions of the leaves, fruits, and seeds of these plants were subjected to antimicrobial testing by the disc diffusion method against 8 clinical isolates of bacteria and 2 strains of fungus. It was found that MC, OT, and FF possessed antimicrobial properties against the test organisms. The MIC for MC ranged from 0.5 to 9 mg/mL and that of FF from 2 to 10 mg/mL and the lowest MIC value (0.5 mg/mL) was recorded for the unripe fruits of MC against E. coli. On the other hand, higher concentration of the unripe MC fruit extract of 9 mg/mL was needed to be effective against a resistant strain of Staphylococcus aureus (MRSA). The antimicrobial effect against MRSA was lost upon ripening of the fruits. The methanolic extract of both MC and FF showed highest MIC values compared to the corresponding aqueous extract, which indicates the low efficacy and the need of higher doses of the plant extract. Phytochemical screening of the plants showed the presence of at least tannins, phenols, flavonoids, and alkaloids, which are known antimicrobial phyto-compounds. In conclusion, the observed antimicrobial properties would tend to further validate the medicinal properties of these commonly used endemic medicinal and food plants of Mauritius.

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

    Directory of Open Access Journals (Sweden)

    Ogah James Ode

    2015-11-01

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

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

    Institute of Scientific and Technical Information of China (English)

    Michael RusselleAlvarez; Francisco Heralde III; Noel Quiming

    2016-01-01

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

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

    Science.gov (United States)

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

    2016-01-01

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

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

    Science.gov (United States)

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

    2016-01-01

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

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

    DEFF Research Database (Denmark)

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

    2015-01-01

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

  16. 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.

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

    Science.gov (United States)

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

    2016-01-01

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

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

    Science.gov (United States)

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

    2016-01-01

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

  19. 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.

  20. Virtual screening of LPXTG competitive SrtA inhibitors targeting signal transduction mechanism in Bacillus anthracis: a combined experimental and theoretical study.

    Science.gov (United States)

    Selvaraj, Chandrabose; Sivakamavalli, Jeyachandran; Baskaralingam, Vaseeharan; Singh, Sanjeev Kumar

    2014-06-01

    Members of the sortase enzyme super family decorate the surfaces of Bacillus anthracis cell wall with proteins that play key roles in microbial pathogenesis and its biofilm formation. Bacillus anthracis Sortase-A (Ba-SrtA) is a potential target for new therapeutics as it is required for B. anthracis survival and replication within macrophages. An understanding of the binding site pocket and substrate recognition mechanism by SrtA enzymes may serve to be beneficial in the rational development of sortase inhibitors. Here, the LPXTG signal peptide-based competitive inhibitors are screened against the Ba-SrtA and compounds with reasonable inhibition, specificity, and mechanisms of inactivation of SrtA have been covered. The screened compounds are experimentally validated against the phylogenetically similar Gram-positive pathogen B. cereus. In situ microscopic visualizations suggest that these screened compounds showed the microbial and biofilm inhibitory activity against B. cereus. It facilitates the further development of these molecules into useful anti-infective agents to treat infections caused by B. anthracis and other Gram-positive pathogens. These results provide insight into basic design principles for generating new clinically relevant lead molecules. It also provides an alternative strategy where a screened ligand molecule can be used in combination to battle increasingly against the Gram-positive pathogens.

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

    Directory of Open Access Journals (Sweden)

    Kai Connie Wu

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

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

    Institute of Scientific and Technical Information of China (English)

    郭书真; 李昌崇; 林立

    2014-01-01

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

  3. Identification of B. anthracis N(5)-carboxyaminoimidazole ribonucleotide mutase (PurE) active site binding compounds via fragment library screening.

    Science.gov (United States)

    Lei, Hao; Jones, Christopher; Zhu, Tian; Patel, Kavankumar; Wolf, Nina M; Fung, Leslie W-M; Lee, Hyun; Johnson, Michael E

    2016-02-15

    The de novo purine biosynthesis pathway is an attractive target for antibacterial drug design, and PurE from this pathway has been identified to be crucial for Bacillus anthracis survival in serum. In this study we adopted a fragment-based hit discovery approach, using three screening methods-saturation transfer difference nucleus magnetic resonance (STD-NMR), water-ligand observed via gradient spectroscopy (WaterLOGSY) NMR, and surface plasmon resonance (SPR), against B. anthracis PurE (BaPurE) to identify active site binding fragments by initially testing 352 compounds in a Zenobia fragment library. Competition STD NMR with the BaPurE product effectively eliminated non-active site binding hits from the primary hits, selecting active site binders only. Binding affinities (dissociation constant, KD) of these compounds varied between 234 and 301μM. Based on test results from the Zenobia compounds, we subsequently developed and applied a streamlined fragment screening strategy to screen a much larger library consisting of 3000 computationally pre-selected fragments. Thirteen final fragment hits were confirmed to exhibit binding affinities varying from 14μM to 700μM, which were categorized into five different basic scaffolds. All thirteen fragment hits have ligand efficiencies higher than 0.30. We demonstrated that at least two fragments from two different scaffolds exhibit inhibitory activity against the BaPurE enzyme.

  4. Drug activity screening based on microsomes-hydrogel system in predicting metabolism induced antitumor effect of oroxylin A.

    Science.gov (United States)

    Yang, Huiying; Li, Jianfeng; Zheng, Yuanting; Zhou, Lu; Tong, Shanshan; Zhao, Bei; Cai, Weimin

    2016-02-24

    A novel microsomes-hydrogel added cell culture system (MHCCS) was employed in the antitumor activity screening of natural compounds, aiming to achieve drug screening with better in vivo correlation, higher initiative to explore the potential active metabolites, and investigation of the antitumor mechanism from the perspective of metabolism. MTT assay and cell apoptosis detection showed that test drug oroxylin A (OA) had enhanced cytotoxicity and wogonin (W) with reduced cytotoxicity on MCF-7 cell line upon MHCCS incubation. In vivo antitumor evaluations also demonstrated that OA induced higher tumor inhibition than W at the same dosage. To explore the reasons, nine major metabolites of OA were separated and collected through UPLC-Q-TOF and semi-preparative HPLC. Metabolites M318 exhibited higher cytotoxicity than OA and other metabolites by MTT assay. (1)H NMR spectrums, HPLC and TOF MS/MS results revealed that OA was catalyzed into its active metabolite M318 via a ring-opening reaction. M318 induced significant cell apoptosis and S-phase arrest through affecting tumor survival related genes after mechanism study. In conclusion, our MHCCS could be a useful tool for drug activity screening from a perspective of metabolism.

  5. High Throughput Screen for Novel Antimicrobials using a Whole Animal Infection Model

    OpenAIRE

    Moy, Terence I.; Annie L Conery; Larkins-Ford, Jonah; Wu, Gang; Mazitschek, Ralph; Casadei, Gabriele; Lewis, Kim; Carpenter, Anne E.; Ausubel, Frederick M.

    2009-01-01

    The nematode Caenorhabditis elegans is a unique whole animal model system for identifying small molecules with in vivo anti-infective properties. C. elegans can be infected with a broad range of human pathogens, including Enterococcus faecalis, an important human nosocomial pathogen with a mortality rate of up to 37% that is increasingly acquiring resistance to antibiotics. Here, we describe an automated, high throughput screen of 37,200 compounds and natural product extracts for those that e...

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

    Science.gov (United States)

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

    2016-08-01

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

  7. Repositioning the substrate activity screening (SAS) approach as a fragment-based method for identification of weak binders.

    Science.gov (United States)

    Gladysz, Rafaela; Cleenewerck, Matthias; Joossens, Jurgen; Lambeir, Anne-Marie; Augustyns, Koen; Van der Veken, Pieter

    2014-10-13

    Fragment-based drug discovery (FBDD) has evolved into an established approach for "hit" identification. Typically, most applications of FBDD depend on specialised cost- and time-intensive biophysical techniques. The substrate activity screening (SAS) approach has been proposed as a relatively cheap and straightforward alternative for identification of fragments for enzyme inhibitors. We have investigated SAS for the discovery of inhibitors of oncology target urokinase (uPA). Although our results support the key hypotheses of SAS, we also encountered a number of unreported limitations. In response, we propose an efficient modified methodology: "MSAS" (modified substrate activity screening). MSAS circumvents the limitations of SAS and broadens its scope by providing additional fragments and more coherent SAR data. As well as presenting and validating MSAS, this study expands existing SAR knowledge for the S1 pocket of uPA and reports new reversible and irreversible uPA inhibitor scaffolds.

  8. Virtual screening of mandelate racemase mutants with enhanced activity based on binding energy in the transition state.

    Science.gov (United States)

    Gu, Jiali; Liu, Min; Guo, Fei; Xie, Wenping; Lu, Wenqiang; Ye, Lidan; Chen, Zhirong; Yuan, Shenfeng; Yu, Hongwei

    2014-02-05

    Mandelate racemase (MR) is a promising candidate for the dynamic kinetic resolution of racemates. However, the poor activity of MR towards most of its non-natural substrates limits its widespread application. In this work, a virtual screening method based on the binding energy in the transition state was established to assist in the screening of MR mutants with enhanced catalytic efficiency. Using R-3-chloromandelic acid as a model substrate, a total of 53 mutants were constructed based on rational design in the two rounds of screening. The number of mutants for experimental validation was brought down to 17 by the virtual screening method, among which 14 variants turned out to possess improved catalytic efficiency. The variant V26I/Y54V showed 5.2-fold higher catalytic efficiency (k(cat)/K(m)) towards R-3-chloromandelic acid than that observed for the wild-type enzyme. Using this strategy, mutants were successfully obtained for two other substrates, R-mandelamide and R-2-naphthylglycolate (V26I and V29L, respectively), both with a 2-fold improvement in catalytic efficiency. These results demonstrated that this method could effectively predict the trend of mutational effects on catalysis. Analysis from the energetic and structural assays indicated that the enhanced interactions between the active sites and the substrate in the transition state led to improved catalytic efficiency. It was concluded that this virtual screening method based on the binding energy in the transition state was beneficial in enzyme rational redesign and helped to better understand the catalytic properties of the enzyme.

  9. Development of a sensitive E-screen assay for quantitative analysis of estrogenic activity in municipal sewage plant effluents.

    Science.gov (United States)

    Körner, W; Hanf, V; Schuller, W; Kempter, C; Metzger, J; Hagenmaier, H

    1999-01-12

    A simplified proliferation test with human estrogen receptor-positive MCF-7 breast cancer cells (E-screen assay) was optimized and validated for the sensitive quantitative determination of total estrogenic activity in effluent samples from municipal sewage plants. After solid phase extraction of 1 l sewage on either 0.2 g polystyrene copolymer (ENV+) or 1 g RP-C18 material and removal of the solvent, analysis of the extracts in the E-screen assay could be performed without any clean-up step. This was even possible with untreated sewage. Parallel extraction of four sewage samples on both different solid phase materials gave comparable quantitative results in the E-screen. A blank sample did not induce cell proliferation. As additive behaviour of the estrogenic response of single compounds was proven for two different mixtures each containing three xenoestrogens, total estrogenic activity in the sewage samples, expressed as 17 beta-estradiol equivalent concentration (EEQ), could be calculated comparing the EC50 values of the samples with those of the positive control 17 beta-estradiol. The detection limit of the E-screen method was 0.05 pmol EEQ/l (0.014 ng EEQ/l), the limit of quantification 0.25-0.5 pmol EEQ/l (0.07-0.14 ng EEQ/l). In total, extracts of nine effluent and one influent sample from five different municipal sewage plants in South Germany were analyzed in the E-screen. All samples strongly induced cell proliferation in a dose-dependent manner which was completely inhibited by coincubation with 5 nM of the estrogen receptor-antagonist ICI 182,780. The proliferative effect relative to the positive control 17 beta-estradiol (RPE) was between 30 and 101%. 17 beta-Estradiol equivalent concentrations were between 2.5 and 25 ng/l indicating a significant input of estrogenic substances via sewage treatment plants into rivers.

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

    Institute of Scientific and Technical Information of China (English)

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

    2005-01-01

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

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

    Science.gov (United States)

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

    2005-08-01

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

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

    OpenAIRE

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

    2015-01-01

    This study investigated the In vitro antiplasmodial activity and phytochemical constituents of the leaves from Alstonia boonei used in the local treatment of malaria. The crude ethanol extract from the medicinal plant (AB-01) was fractionated into ethyl acetate (AB-01-01), chloroform (AB-01-02) and n-hexane (AB-01-03) fractions. In vitro antiplasmodial assays and phytochemical screening of ethyl acetate, chloroform and n-hexane fractions from the plant were further carried out. Alkaloids, sap...

  13. 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.

  14. Screening for Anthelminthic Activities from Extracts of Zanthoxylum Zanthoxyloides, Neocarya Macrophylla and Celosia Laxa Against Ascaris Infection in Rabbits

    Directory of Open Access Journals (Sweden)

    B B Barnabas

    2010-12-01

    Full Text Available Summary: Extracts of Celosia laxa, Neocarya macrophylla and Zanthoxylum zanthoxyloides leaves were screened for anthelminthic activities on Ascaris lumbricoides. Celosia laxa appeared to be more potent against A. lumbricoides with rapid recovery of weight while Z. zanthoxyloides has the lowest potency. The effects of these plant extracts on Ascaris lumbricoides suggest that they could serve as an alternative source of anthelminthic agent. Industrial relevance: Infectious diseases pose serious challenges to global health care delivery. Moreoever, in developing countries, the cost of orthodox medication is out of reach of the common man, especially those in rural areas. This is coupled with the adulterated drugs and emergences of drug resistant strains have led to an intensive search for natural products of higher plants, which are biologically active against parasitic infections. Many plants are used locally in traditional medicine to treat parasitic infections. Nigeria offers a rich floral diversity that are used traditionally to treat worm infections. Nigerian medicinal plants (Celosia laxa, Neocarya macrophylla, Zanthoxylum zanthoxyloides used commonly used in Bida, Niger State, Nigeria for the treatment of worm infections were screened for anthelminthic activity. The extracts exhibited varying degree of anthelminthic activities against Ascaris lumbricoides. The extract of C. laxa display potent anthelminthic property. The extract of C. laxa with pronounced activity against A. lumbricoides may contain metabolites that have pharmacologically active principles with promising anthelminthic properties. This indicates the medical potential of C. laxa in the treatment of helminthiasis.

  15. 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.

  16. Screening of phytochemicals and antimicrobial activity of Caulerpa scalpelliformis collected from Manapad Coast, Tuticorin District, Tamilnadu, South India

    Institute of Scientific and Technical Information of China (English)

    N Karthick; M Anees Fathimal; K Ramesh; H Sridhar; M Natrajan; VV Divya; M Umavanitha; S Umamaheswari

    2014-01-01

    Objective:To analyse the phytochemicals, elements and evaluate the antimicrobial activity of Caulerpa scalpelliformis (C. scalpelliformis) against different bacterial and fungal pathogens. Methods: For the elemental analysis and the screening of phytochemicals, some common and available standard tests were done. The antimicrobial activity was done through the agar well diffusion method. Results:In the qualitative phytochemical screening, among the five different solvent extracts of C. scalpelliformis, the benzene extract showed a maximum number of compounds such as tannins, flavanoids, glycosides, phenols, saponins, terpenoids, etc. The quantitative analysis showed the total protein, total carbohydrate and total lipid content to be (15.86±1.13)%w/w, (10.32±0.94)%w/w, and (1.05±0.08)% w/w respectively. The antibacterial activity showed a maximum zone of inhibition (15±0.18) mm and a minimum zone of inhibition (6±0.05) mm in the benzene extract of C. scalpelliformis exhibited against Serratia marcescens and Bacillus subtilis. The antifungal assay of C. scalpelliformis showed the benzene extract rendered a maximum activity (20±0.25) mm against Aspergillus terreus whereas a minimum activity (12±0.14) mm obtained in the chloroform extract against Aspergillus flavus. Conclusions: Our findings provide the evidence that the benzene extract of C. scalpelliformis possesses the good antimicrobial activity and hence the algae proves to be an effective therapeutic agent.

  17. T-Screen as a tool to identify thyroid hormone receptor active compounds

    NARCIS (Netherlands)

    Gutleb, A.C.; Meerts, I.A.T.M.; Bergsma, J.H.; Schriks, M.; Murk, A.J.

    2005-01-01

    The T-Screen represents an in vitro bioassay based on thyroid hormone dependent cell proliferation of a rat pituitary tumour cell line (GH3) in serum-free medium. It can be used to study interference of compounds with thyroid hormone at the cellular level, thus bridging the gap between limitations o

  18. 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.

  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...

  20. Antifungal activity and phytochemical screening of extracts from Phoenix dactylifera L. cultivars.

    Science.gov (United States)

    Boulenouar, Noureddine; Marouf, Abderrazak; Cheriti, Abdelkrim

    2011-12-01

    In this study, the rachis extracts of eight date palm Phoenix dactylifera L. cultivars were analysed by phytochemical screening and bioautography on Fusarium oxysporum f. sp. albedinis (Foa). The choice of cultivars was based on their reaction to Foa (resistant, tolerant and sensitive). Phytochemical screening was realised for flavonoids, tannins, alkaloids and coumarins. Antifungal effects were mostly represented by dichloromethanic extracts (seven out of nine inhibition zones). The best results were represented by the dichloromethanic extract of the cultivar 'Bent-Cherk' rachis (6.50 ± 1.41 mm) and the ethyl acetate extract of the cultivar 'Rotbi' rachis (6.00 ± 1.41 mm). The date palm cultivars presented some similarities concerning phytochemical screening results related to their resistance or sensibility to Foa. From the correlation between phytochemical screening and bioautography, it was observed that the majority of bioactive compounds against Foa seem to be polyphenols. Thus, the natural defence mechanism in vivo against Foa is probably related to the action of polyphenols. The difference between resistant, tolerant and sensitive cultivars is related to their mechanism of action.

  1. Development of potent anti-infective agents from Silurana tropicalis: conformational analysis of the amphipathic, alpha-helical antimicrobial peptide XT-7 and its non-haemolytic analogue [G4K]XT-7.

    Science.gov (United States)

    Subasinghage, Anusha P; Conlon, J Michael; Hewage, Chandralal M

    2010-04-01

    Peptide XT-7 (GLLGP(5)LLKIA(10)AKVGS(15)NLL.NH(2)) is a cationic, leucine-rich peptide, first isolated from skin secretions of the frog, Silurana tropicalis (Pipidae). The peptide shows potent, broad-spectrum antimicrobial activity but its therapeutic potential is limited by haemolytic activity (LC(50)=140 microM). The analogue [G4K]XT-7, however, retains potent antimicrobial activity but is non-haemolytic (LC(50)>500 microM). In order to elucidate the molecular basis for this difference in properties, the three dimensional structures of XT-7 and the analogue have been investigated by proton NMR spectroscopy and molecular modelling. In aqueous solution, both peptides lack secondary structure. In a 2,2,2-trifluoroethanol (TFE-d(3))-H(2)O mixed solvent system, XT-7 is characterised by a right handed alpha-helical conformation between residues Leu(3) and Leu(17) whereas [G4K]XT-7 adopts a more restricted alpha-helical conformation between residues Leu(6) and Leu(17). A similar conformation for XT-7 in 1,2-dihexanoyl-sn-glycero-3-phosphocholine (DHPC) micellular media was observed with a helical segment between Leu(3) and Leu(17). However, differences in side chain orientations restricting the hydrophilic residues to a smaller patch resulted in an increased hydrophobic surface relative to the conformation in TFE-H(2)O. Molecular modelling of the structures obtained in our study demonstrates the amphipathic character of the helical segments. It is proposed that the marked decrease in haemolytic activity produced by the substitution Gly(4)-->Lys in XT-7 arises from a decrease in both helicity and hydrophobicity. These studies may facilitate the development of potent but non-toxic anti-infective agents based upon the structure of XT-7.

  2. 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.

  3. 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.

  4. BIOCHEMICAL GENETIC STUDIES ON CUTYLEFISH SEPIELLA MAINDRONI (CEPHALOPODA: SEPIIDAE)——ACTIVE LOCI SCREENING OF ISOZYME

    Institute of Scientific and Technical Information of China (English)

    郑小东; YutakaNatsukari; 王如才; 王昭萍; 李云

    2001-01-01

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

  5. EVALUATION OF ANTIOXIDANT ACTIVITY AND PHYTOCHEMICAL SCREENING OF MALUS DOMESTICA BORKH (APPLE AND PHASEOLUS VULGARIS L. (GREEN BEANS

    Directory of Open Access Journals (Sweden)

    A.Doss

    2012-06-01

    Full Text Available The aim of this study was to determine the antioxidant activity as well as total phenol (TPC and total flavonoid content (TFC in two fruits, apple (Malus domestica and green beans (Phaseolus vulgaris. The antioxidant activities were examined by two different methods namely DPPH free radical scavenging activity and reducing power scavenging activity. The results showed that considerable amount of TPC and TFC was present in these fruit extracts as well as these vegetables contain a vast array of different phytochemicals in their dry form. Apple showed higher antioxidant activity than green beans. Phytochemical screening revealed the presence of saponins, steroids, flavonoids and carbohydrates & glycosides in all the extracts. Overall, the present results provided basic data for choosing these fruits with high antioxidant capacity for consumption or for the development of antioxidant based medicines as value-added products.

  6. [Inhalation therapy: inhaled generics, inhaled antidotes, the future of anti-infectives and the indications of inhaled pentamidine. GAT aerosolstorming, Paris 2012].

    Science.gov (United States)

    Peron, N; Le Guen, P; Andrieu, V; Bardot, S; Ravilly, S; Oudyi, M; Dubus, J-C

    2013-12-01

    The working group on aerosol therapy (GAT) of the Société de pneumologie de langue française (SPLF) organized its third "Aerosolstorming" in 2012. During the course of one day, different aspects of inhaled therapy were discussed, and these will be treated separately in two articles, this one being the first. Inhaled products represent a large volume of prescriptions both in the community and in hospital settings and they involve various specialties particularly ENT and respiratory care. Technical aspects of the development of these products, their mode of administration and compliance with their indications are key elements for the effective therapeutic use of inhaled treatments. In this first article, we will review issues concerning generic inhaled products, the existence of inhaled antidotes, new anti-infective agents and indications for inhaled pentamidine.

  7. New classes of alanine racemase inhibitors identified by high-throughput screening show antimicrobial activity against Mycobacterium tuberculosis.

    Directory of Open Access Journals (Sweden)

    Karen G Anthony

    Full Text Available BACKGROUND: In an effort to discover new drugs to treat tuberculosis (TB we chose alanine racemase as the target of our drug discovery efforts. In Mycobacterium tuberculosis, the causative agent of TB, alanine racemase plays an essential role in cell wall synthesis as it racemizes L-alanine into D-alanine, a key building block in the biosynthesis of peptidoglycan. Good antimicrobial effects have been achieved by inhibition of this enzyme with suicide substrates, but the clinical utility of this class of inhibitors is limited due to their lack of target specificity and toxicity. Therefore, inhibitors that are not substrate analogs and that act through different mechanisms of enzyme inhibition are necessary for therapeutic development for this drug target. METHODOLOGY/PRINCIPAL FINDINGS: To obtain non-substrate alanine racemase inhibitors, we developed a high-throughput screening platform and screened 53,000 small molecule compounds for enzyme-specific inhibitors. We examined the 'hits' for structural novelty, antimicrobial activity against M. tuberculosis, general cellular cytotoxicity, and mechanism of enzyme inhibition. We identified seventeen novel non-substrate alanine racemase inhibitors that are structurally different than any currently known enzyme inhibitors. Seven of these are active against M. tuberculosis and minimally cytotoxic against mammalian cells. CONCLUSIONS/SIGNIFICANCE: This study highlights the feasibility of obtaining novel alanine racemase inhibitor lead compounds by high-throughput screening for development of new anti-TB agents.

  8. Comparative analysis of tertiary alcohol esterase activity in bacterial strains isolated from enrichment cultures and from screening strain libraries.

    Science.gov (United States)

    Herter, Susanne; Nguyen, Giang-Son; Thompson, Mark L; Steffen-Munsberg, Fabian; Schauer, Frieder; Bornscheuer, Uwe T; Kourist, Robert

    2011-05-01

    The preparation of enantiopure tertiary alcohols is of great contemporary interest due to the application of these versatile building blocks in organic synthesis and as precursors towards high value pharmaceutical compounds. Herein, we describe two approaches taken towards the discovery of novel biocatalysts for the synthesis of these valuable compounds. The first approach was initiated with screening of 47 bacterial strains for hydrolytic activity towards the simple tertiary alcohol ester tert-butyl acetate. In conjunction, a second method focussed on the isolation of strains competent for growth on tert-butyl acetate as the sole source of carbon and energy. From functional screening, 10 Gram-positive Actinomycetes showed hydrolytic activity, whilst enrichment selection resulted in the identification of 14 active strains, of which five belong to the Gram-negative cell-wall type. Bacterial strains obtained from both approaches were viable for enantioselective hydrolysis of pyridine substituted tertiary alcohol esters in addition to bulky aliphatic and keto-derived substrates from the same class. Activity towards each of the test substrates was uncovered, with promising enantioselectivities of up to E = 71 in the hydrolysis of a para-substituted pyridine tertiary alcohol ester using a strain of Rhodococcus ruber. Interestingly strains of Microbacterium and Alcaligenes sp. gave opposite enantiopreference in the hydrolysis of a meta-substituted pyridine tertiary alcohol ester with E values of 17 and 54. These approaches show that via both possibilities, screening established strain collections and performing enrichment selection, it is possible to identify novel species which show activity towards sterically challenging substrates.

  9. Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.

    Science.gov (United States)

    Kym, Philip R; Souers, Andrew J; Campbell, Thomas J; Lynch, John K; Judd, Andrew S; Iyengar, Rajesh; Vasudevan, Anil; Gao, Ju; Freeman, Jennifer C; Wodka, Dariusz; Mulhern, Mathew; Zhao, Gang; Wagaw, Seble H; Napier, James J; Brodjian, Sevan; Dayton, Brian D; Reilly, Regina M; Segreti, Jason A; Fryer, Ryan M; Preusser, Lee C; Reinhart, Glenn A; Hernandez, Lisa; Marsh, Kennan C; Sham, Hing L; Collins, Christine A; Polakowski, James S

    2006-04-06

    An inactin-anesthetized rat cardiovascular (CV) assay was employed in a screening mode to triage multiple classes of melanin-concentrating hormone receptor 1 (MCHr1) antagonists. Lead identification was based on a compound profile producing high drug concentration in both plasma (>40 microM) and brain (>20 microg/g) with optimization activities on multiple classes of MCHr1 antagonists were terminated. After providing evidence that the cardiovascular liabilities were not a function of MCHr1 antagonism, continued screening identified the chromone-substituted aminopiperidine amides as a class of MCHr1 antagonists that demonstrated a safe cardiovascular profile at high drug concentrations in both plasma and brain. The high incidence of adverse cardiovascular effects associated with an array of MCHr1 antagonists of significant chemical diversity, combined with the stringent safety requirements for antiobesity drugs, highlight the importance of incorporating cardiovascular safety assessment early in the lead selection process.

  10. Soluble urokinase plasminogen activator receptor as a prognostic marker in men participating in prostate cancer screening

    DEFF Research Database (Denmark)

    Kjellman, A; Akre, O; Gustafsson, O;

    2011-01-01

    with prostate cancer and cardiovascular disease mortality. METHODS: Using time-resolved fluorescence immunoassays, we measured intact suPAR [suPAR(I-III)] and intact plus cleaved suPAR [suPAR(I-III) + suPAR(II-III)] and thus calculated the amount of suPAR(II-III) in serum samples from 375 men participating...... cardiovascular disease. No similar association was found for prostate cancer after adjustment for other prognostic factors....... 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...

  11. Phytochemical screening and antioxidant activity of seven Medicinal plants species from Ecuador

    OpenAIRE

    García García, Isabel Josefa

    2015-01-01

    Seven plant species, used as traditional medicine, from two regions of Ecuador have been subjected to qualitative and cuantitative phytochemistry screening in order to provide information about possible chemical compounds present in these species that will contribute to future researchs. Chuquiraga jussieui J.F. Gmel., Pseudognaphalium elegans (Kunth) Kartesz (Asteraceae), Gustavia pubescens Ruiz & Pav. ex Berg (Lecythidaceae), Aeghiphila alba Moldenke (Lamiaceae), Cleome spinosa Jacq. (Cleom...

  12. A High-affinity Activator of G551D-CFTR Chloride Channel Identified By High Throughput Screening

    Institute of Scientific and Technical Information of China (English)

    ZHAO Lu; HE Cheng-yan; LIU Yan-li; ZHOU Hong-lan; ZHOU Jin-song; SHANG De-jing; YANG Hong

    2004-01-01

    A stably transfected CHO cell line coexpressing G551D-CFTR and iodide-sensitive yellow fluorescent protein mutant EYFP-H148Q-I152L was successfully established and used as assay model to identify small-molecule activators of G551D-CFTR chloride channel from 100000 diverse combinatorial compounds by high throughput screening on a customized Beckman robotic system. A bicyclooctane compound was identified to activate G551D-CFTR chloride channel with high-affinity(Kd=1.8 μmol/L). The activity of the bicyclooctane compound is G551D-CFTR-specific, reversible and non-toxic. The G551D-CFTR activator may be useful as a tool to study the mutant G551D-CFTR chloride channel structure and transport properties and as a candidate drug to cure cystic fibrosis caused by G551D-CFTR mutation.

  13. Pharmacophore-based virtual screening, biological evaluation and binding mode analysis of a novel protease-activated receptor 2 antagonist

    Science.gov (United States)

    Cho, Nam-Chul; Seo, Seoung-Hwan; Kim, Dohee; Shin, Ji-Sun; Ju, Jeongmin; Seong, Jihye; Seo, Seon Hee; Lee, Iiyoun; Lee, Kyung-Tae; Kim, Yun Kyung; No, Kyoung Tai; Pae, Ae Nim

    2016-08-01

    Protease-activated receptor 2 (PAR2) is a G protein-coupled receptor, mediating inflammation and pain signaling in neurons, thus it is considered to be a potential therapeutic target for inflammatory diseases. In this study, we performed a ligand-based virtual screening of 1.6 million compounds by employing a common-feature pharmacophore model and two-dimensional similarity search to identify a new PAR2 antagonist. The common-feature pharmacophore model was established based on the biological screening results of our in-house library. The initial virtual screening yielded a total number of 47 hits, and additional biological activity tests including PAR2 antagonism and anti-inflammatory effects resulted in a promising candidate, compound 43, which demonstrated an IC50 value of 8.22 µM against PAR2. In next step, a PAR2 homology model was constructed using the crystal structure of the PAR1 as a template to explore the binding mode of the identified ligands. A molecular docking method was optimized by comparing the binding modes of a known PAR2 agonist GB110 and antagonist GB83, and applied to predict the binding mode of our hit compound 43. In-depth docking analyses revealed that the hydrophobic interaction with Phe2435.39 is crucial for PAR2 ligands to exert antagonistic activity. MD simulation results supported the predicted docking poses that PAR2 antagonist blocked a conformational rearrangement of Na+ allosteric site in contrast to PAR2 agonist that showed Na+ relocation upon GPCR activation. In conclusion, we identified new a PAR2 antagonist together with its binding mode, which provides useful insights for the design and development of PAR2 ligands.

  14. Pharmacophore-based virtual screening, biological evaluation and binding mode analysis of a novel protease-activated receptor 2 antagonist.

    Science.gov (United States)

    Cho, Nam-Chul; Seo, Seoung-Hwan; Kim, Dohee; Shin, Ji-Sun; Ju, Jeongmin; Seong, Jihye; Seo, Seon Hee; Lee, Iiyoun; Lee, Kyung-Tae; Kim, Yun Kyung; No, Kyoung Tai; Pae, Ae Nim

    2016-08-01

    Protease-activated receptor 2 (PAR2) is a G protein-coupled receptor, mediating inflammation and pain signaling in neurons, thus it is considered to be a potential therapeutic target for inflammatory diseases. In this study, we performed a ligand-based virtual screening of 1.6 million compounds by employing a common-feature pharmacophore model and two-dimensional similarity search to identify a new PAR2 antagonist. The common-feature pharmacophore model was established based on the biological screening results of our in-house library. The initial virtual screening yielded a total number of 47 hits, and additional biological activity tests including PAR2 antagonism and anti-inflammatory effects resulted in a promising candidate, compound 43, which demonstrated an IC50 value of 8.22 µM against PAR2. In next step, a PAR2 homology model was constructed using the crystal structure of the PAR1 as a template to explore the binding mode of the identified ligands. A molecular docking method was optimized by comparing the binding modes of a known PAR2 agonist GB110 and antagonist GB83, and applied to predict the binding mode of our hit compound 43. In-depth docking analyses revealed that the hydrophobic interaction with Phe243(5.39) is crucial for PAR2 ligands to exert antagonistic activity. MD simulation results supported the predicted docking poses that PAR2 antagonist blocked a conformational rearrangement of Na(+) allosteric site in contrast to PAR2 agonist that showed Na(+) relocation upon GPCR activation. In conclusion, we identified new a PAR2 antagonist together with its binding mode, which provides useful insights for the design and development of PAR2 ligands.

  15. ANTIMICROBIAL ACTIVITIES AND PRELIMINARY PHYTOCHEMICAL SCREENING ON THE CRUDE EXTRACTS OF THE LEAVES OF CINERARIA ABYSSINICA SCH. BIP. EXA. RICH

    Directory of Open Access Journals (Sweden)

    Biruk Sintayehu*, Kaleab Asres and Avijit Mazumder

    2012-05-01

    Full Text Available In Ethiopian traditional medicine, the aqueous decoction of the leaves of Cineraria abyssinica Sch. Bip. exA. Rich (Asteraceae is used for treatments of various ailments including diarrhea, however, to date, there appear to have been no reports on the phytochemistry and the antimicrobial activity of the plant. The main aim of this study was, therefore, to carry out preliminary phytochemical screening and antimicrobial activities on leaf extracts of C. abyssinica. The in vitro antimicrobial activities of the aqueous and 80% methanolic crude extracts of the leaves of C. abyssinica were investigated against Gram positive and Gram negative bacteria by agar disc diffusion method. Both the aqueous and 80% methanolic extracts showed various degrees of potent antibacterial activities comparable to the standard drug ciprofloxacin against all of the bacteria tested except Bacillus species. Preliminary phytochemical screening of the plant revealed the presence of polyphenols, flavonoids, coumarins, saponins, terpenoids and phytosterols. The acute toxicity studies showed the nontoxic nature of the plant up to 3 g/kg. Therefore, the present study revealed for the first time the presence of antimicrobial phytochemicals in the leaves of C. abyssinica that scientifically validated the traditional use and its great potential to be used for treatment of infectious diarrhea.

  16. 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

  17. 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; 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 nor...

  18. Screen time and children

    Science.gov (United States)

    ... obesity ) Screen time increases your child's risk of obesity because: Sitting and watching a screen is time that is not spent being physically active. TV commercials and other screen ads can lead to unhealthy food choices . Most of the time, the foods in ads ...

  19. 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 produc

  20. Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.

    Directory of Open Access Journals (Sweden)

    Gregory J Crowther

    Full Text Available In 2010 the identities of thousands of anti-Plasmodium compounds were released publicly to facilitate malaria drug development. Understanding these compounds' mechanisms of action--i.e., the specific molecular targets by which they kill the parasite--would further facilitate the drug development process. Given that kinases are promising anti-malaria targets, we screened ~14,000 cell-active compounds for activity against five different protein kinases. Collections of cell-active compounds from GlaxoSmithKline (the ~13,000-compound Tres Cantos Antimalarial Set, or TCAMS, St. Jude Children's Research Hospital (260 compounds, and the Medicines for Malaria Venture (the 400-compound Malaria Box were screened in biochemical assays of Plasmodium falciparum calcium-dependent protein kinases 1 and 4 (CDPK1 and CDPK4, mitogen-associated protein kinase 2 (MAPK2/MAP2, protein kinase 6 (PK6, and protein kinase 7 (PK7. Novel potent inhibitors (IC50 < 1 μM were discovered for three of the kinases: CDPK1, CDPK4, and PK6. The PK6 inhibitors are the most potent yet discovered for this enzyme and deserve further scrutiny. Additionally, kinome-wide competition assays revealed a compound that inhibits CDPK4 with few effects on ~150 human kinases, and several related compounds that inhibit CDPK1 and CDPK4 yet have limited cytotoxicity to human (HepG2 cells. Our data suggest that inhibiting multiple Plasmodium kinase targets without harming human cells is challenging but feasible.

  1. 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.

  2. 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.

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

    Directory of Open Access Journals (Sweden)

    Bitasta Mandal

    2013-05-01

    Full Text Available Stevia rebaudiana Bertoni, a natural non-caloric substitute to conventional sugar, is also popular as the “sweet herb of Paraguay”. It is a storehouse of various bioactive constituents mainly, the ent-kaurene diterpene glycosides namely stevioside, rebaudioside A, B, C, D and E. The plant is known to exhibit a wide range of biological activities like hypoglycemic, anti-oxidant, anticancer, antibacterial activities. The present research is based on a preliminary phytochemical screening and comparative evaluation of in vitro antioxidant activity of the dried leaves of five varieties of Stevia rebaudiana procured from five different geographical locations of India viz., Delhi, Surat, Kangra, Bangalore and Indore. Total phenolic and total flavonoid content was also determined using Folin-Ciocalteu reagent method and aluminum chloride colorimetric. The result showed that the variety from Kangra showed the highest phenolic and flavonoid content of 5.87 and 62.22 mg GAE/L respectively.

  4. [SCREENING OF WILD SPREAD AND CULTIVATED OF BUXUS SPECIES GROWING IN GEORGIA ON THE CONTENT OF ALKALOIDS AND BIOLOGICAL ACTIVITY].

    Science.gov (United States)

    Vachnadze, N; Mchedlidze, Q; Novikova, J; Suladze, T; Vachnadze, V

    2016-07-01

    Georgian flora is represented by about 4150 plant species. Many important alkaloid-containing plant species and among of them are species Buxus L. of genus in Adjara. The aims of the research were: sequential screening of the plants for the consistence of alkaloids; Study of anatomical characteristics of Buxus colchica Pojark. and revealing of specific pharmacological activity of steroidal alkaloids. The objects of research were B. colchica, B. balearika and B. sempervirens, growing in Adjara (Georgia), collected in active phase of flowering of the plants. There were revealed 370 species of alkaloid containing plants. Sum of alkaloids and crude aqueous extract have spasmolitic and antihistaminic activity. Experimental anatomical research of diagnostic characteristics of the bines showed the existence of monocyclic transient system with fiber like tracheids, dorsoventral mesophyll of the leaves; the structure for the upper part of epidermis is linear and the lower part is curved, type of stomata is paracitic.

  5. Sulphonamide and sulphonyl-hydrazone cyclic imide derivatives: antinociceptive activity, molecular modeling and in silico ADMET screening.

    Science.gov (United States)

    de Oliveira, Kely N; Souza, Márcia M; Sathler, Plínio Cunha; Magalhães, Uiaran O; Rodrigues, Carlos R; Castro, Helena C; Palm, Patrícia R; Sarda, Maicon; Perotto, Pablo E; Cezar, Sabrina; de Brito, Monique A; Ferreira, Ariane S S R; Cabral, Lúcio Mendes; Machado, Clodoaldo; Nunes, Ricardo J

    2012-10-01

    In this paper, we describe the antinociceptive activity, molecular modeling and in silico ADMET screening of a series of sulphonyl-hydrazone and sulphonamide imidobenzene derivatives. Among these compounds, the sulphonyl-hydrazones 9 and 11 showed the most potent analgesic activity (ID(50) = 5.1 and 6.8 μmol/kg, respectively). Interestingly, all derivatives evaluated in this study have a better analgesic profile than the control drugs, acetyl salicylic acid and acetaminophen. Derivative 9 was the most promising compound; with a level of activity that was 24 times higher than the control drugs. Our SAR study showed a relationship among the distribution of the frontier orbital HOMO coefficients, HOMO-LUMO energy gap of these molecules and their reactivity. The best analgesic compounds (including 6, 9, 10, 11 and 12) fulfilled the Lipinski "rule-of-five", which is theoretically important for good drug absorption and permeation.

  6. 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

  7. 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.

  8. 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.

  9. 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.

  10. 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

  11. PDCA循环理论用于抗感染临床药师工作模式实践%PDCA Cycle Theory in the Role of Anti-Infective Clinical Pharmacists Working Mode

    Institute of Scientific and Technical Information of China (English)

    王莉; 王娜; 张伟东; 杨文明; 贾俐萍; 马金秋; 董建红; 左明芳; 祖香雨

    2015-01-01

    Objective To explore the role of the plan,do,check and action(PDCA) theory in the establishment of the anti-infective clinical pharmacists work mode. Methods With the PDCA quality cycle management theory as the guidance,the clinical pharmacists work systems and work processes were established for standardizing the clinical pharmacists' works. Results The working systems and workflow formulated by the PDCA mode could effectively enhance the work level and work quality of clinical pharmacists. Conclusion The PDCA cycle theory plays an active role for constructing clinical pharmacists work mode and significantly increases the work level of hospital clinical pharmacists.%目的:探讨戴明环(PDCA)循环理论在建立抗感染临床药师工作模式中的作用。方法以PDCA质量循环管理理论为指导,建立临床药师工作制度和工作流程,使临床药师工作标准化。结果通过PDCA模式制订的工作制度和工作流程能有效提升临床药师的工作水平和工作质量。结论 PDCA循环理论对构建临床药师工作模式起到了积极作用,明显提高了医院临床药师的工作水平。

  12. 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.

  13. Research Advances of Aminoacyl-tRNA Synthetase Inhibitors as Novel Anti-infective Agents%氨酰tRNA合成酶抑制剂作为新型抗感染药物的研究进展

    Institute of Scientific and Technical Information of China (English)

    王庆; 孟青青; 周虎臣

    2012-01-01

    Increasing rates of bacterial resistance to known classes of antibiotics present a severe global challenge. As a consequence, the search for new chemical entities that address novel bacterial targets remains ongoing. Aminoacyl-tRNA synthetases (aaRS) catalyze the ligation of amino acids to their cognate tRNAs and they are essential for protein synthesis. Inhibition of aaRS leads to protein synthesis inhibition, which cause cell growth arrest. Consequently, aminoacyl-tRNA synthetase is a class of potential anti-infective target. AaRS inhibitors identified from natural products and their derivatives, substrate and reaction intermediate mimics, synthetic compounds and hits of virtual screening as novel antibacterial and antifungal agents are summarized in this article. The target characteristic, classification and catalytic mechanism of aminoacyl-tRNA synthetases are also introduced.%细菌耐药性的不断上升对现有阶段的抗生素类药物提出了一个严峻的挑战,同时也掀起了针对于新靶标的抗菌药物的研究.氨酰tRNA合成酶(aaRS)催化特定氨基酸连接到相应的tRNA分子上,在蛋白质的合成过程中起着必不可少的作用.氨酰tRNA合成酶的抑制会导致蛋白质合成的停止,扰乱细菌和真菌的生长,因此氨酰tRNA合成酶是一类潜在的抗感染靶标.本文分别综述了天然产物及其衍生的aaRS抑制剂,底物和反应中间体模拟物,通过合成和通过虚拟筛选得到的aaRS抑制剂作为新型抗细菌和抗真菌药物的研究进展,并对aaRS的靶标特点、分类和催化机制作一简要介绍.

  14. Synthetic Lethality Screen Identifies RPS6KA2 as Modifier of Epidermal Growth Factor Receptor Activity in Pancreatic Cancer

    Directory of Open Access Journals (Sweden)

    Nada Milosevic

    2013-12-01

    Full Text Available Pancreatic cancer is characterized by a high degree of resistance to chemotherapy. Epidermal growth factor receptor (EGFR inhibition using the small-molecule inhibitor erlotinib was shown to provide a small survival benefit in a subgroup of patients. To identify kinases whose inhibition acts synergistically with erlotinib, we employed a kinome-wide small-interfering RNA (siRNA-based loss-of-function screen in the presence of erlotinib. Of 779 tested kinases, we identified several targets whose inhibition acted synergistically lethal with EGFR inhibition by erlotinib, among them the S6 kinase ribosomal protein S6 kinase 2 (RPS6KA2/ribosomal S6 kinase 3. Activated RPS6KA2 was expressed in approximately 40% of 123 human pancreatic cancer tissues. RPS6KA2 was shown to act downstream of EGFR/RAS/mitogen-activated protein kinase kinase (MEK/extracellular-signal regulated kinase (ERK signaling and was activated by EGF independently of the presence of KRAS mutations. Knockdown of RPS6KA2 by siRNA led to increased apoptosis only in the presence of erlotinib, whereas RPS6KA2 activation or overexpression rescued from erlotinib- and gemcitabine-induced apoptosis. This effect was at least in part mediated by downstream activation of ribosomal protein S6. Genetic as well as pharmacological inhibition of RPS6KA2 by the inhibitor BI-D1870 acted synergistically with erlotinib. By applying this synergistic lethality screen using a kinome-wide RNA interference-library approach, we identified RPS6KA2 as potential drug target whose inhibition synergistically enhanced the effect of erlotinib on tumor cell survival. This kinase therefore represents a promising drug candidate suitable for the development of novel inhibitors for pancreatic cancer therapy.

  15. Functionalized Carbon Quantum Dots with Dopamine for Tyrosinase Activity Monitoring and Inhibitor Screening: In Vitro and Intracellular Investigation.

    Science.gov (United States)

    Chai, Lujing; Zhou, Jin; Feng, Hui; Tang, Cong; Huang, Yuanyuan; Qian, Zhaosheng

    2015-10-28

    Sensitive assay of tyrosinase (TYR) activity is in urgent demand for both fundamental research and practical application, but the exploration of functional materials with good biocompatibility for its activity evaluation at the intracellular level is still challenging until now. In this work, we develop a convenient and real-time assay with high sensitivity for TYR activity/level monitoring and its inhibitor screening based on biocompatible dopamine functionalized carbon quantum dots (Dopa-CQDs). Dopamine with redox property was functionalized on the surface of carbon quantum dots to construct a Dopa-CQDs conjugate with strong bluish green fluorescence. When the dopamine moiety in Dopa-CQDs conjugate was oxidized to a dopaquinone derivative under specific catalysis of TYR, an intraparticle photoinduced electron transfer (PET) process between CQDs and dopaquinone moiety took place, and then the fluorescence of the conjugate could be quenched simultaneously. Quantitative evaluation of TYR activity was established in terms of the relationship between fluorescence quenching efficiency and TYR activity. The assay covered a broad linear range of up to 800 U/L with a low detection limit of 7.0 U/L. Arbutin, a typical inhibitor of TYR, was chosen as an example to assess its function of inhibitor screening, and positive results were observed that fluorescence quenching extent of the probe was reduced in the presence of arbutin. It is also demonstrated that Dopa-CQD conjugate possesses excellent biocompatibility, and can sensitively monitor intracellular tyrosinase level in melanoma cells and intracellular pH changes in living cells, which provides great potential in application of TYR/pH-associated disease monitoring and medical diagnostics.

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

    Directory of Open Access Journals (Sweden)

    Nabila Benariba

    2013-01-01

    Conclusions: These qualitative and quantitative analytical data document the presence in C. colocynthis extracts of such chemical compounds as flavonoids responsible for the antioxidant activity, as well as other biological activities of this plant.

  17. 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...

  18. Physical Activity in Patients with Metabolic Syndrome: At Screening and 3 Years Thereafter

    NARCIS (Netherlands)

    Jansen, H.; Engelsen, C. den; Rutten, G.E.H.M.

    2013-01-01

    Background: Metabolic syndrome is a cluster of risk factors for cardiovascular disease and type 2 diabetes. Physical activity can decrease these risks. Many randomized clinical trials to increase physical activity have demonstrated disappointing results, and implementation in daily practice appeared

  19. DNA-conjugated gold nanoparticles based colorimetric assay to assess helicase activity: a novel route to screen potential helicase inhibitors

    Science.gov (United States)

    Deka, Jashmini; Mojumdar, Aditya; Parisse, Pietro; Onesti, Silvia; Casalis, Loredana

    2017-03-01

    Helicase are essential enzymes which are widespread in all life-forms. Due to their central role in nucleic acid metabolism, they are emerging as important targets for anti-viral, antibacterial and anti-cancer drugs. The development of easy, cheap, fast and robust biochemical assays to measure helicase activity, overcoming the limitations of the current methods, is a pre-requisite for the discovery of helicase inhibitors through high-throughput screenings. We have developed a method which exploits the optical properties of DNA-conjugated gold nanoparticles (AuNP) and meets the required criteria. The method was tested with the catalytic domain of the human RecQ4 helicase and compared with a conventional FRET-based assay. The AuNP-based assay produced similar results but is simpler, more robust and cheaper than FRET. Therefore, our nanotechnology-based platform shows the potential to provide a useful alternative to the existing conventional methods for following helicase activity and to screen small-molecule libraries as potential helicase inhibitors.

  20. A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor

    Science.gov (United States)

    Ackerknecht, Sabine; Lehembre, François; Fink, Tobias; Stritt, Manuel; Wirth, Matthias; Pavan, Simona; Bill, Ruben; Regenass, Urs; Christofori, Gerhard; Meyer-Schaller, Nathalie

    2016-01-01

    An epithelial to mesenchymal transition (EMT) enables epithelial tumor cells to break out of the primary tumor mass and to metastasize. Understanding the molecular mechanisms driving EMT in more detail will provide important tools to interfere with the metastatic process. To identify pharmacological modulators and druggable targets of EMT, we have established a novel multi-parameter, high-content, microscopy-based assay and screened chemical compounds with activities against known targets. Out of 3423 compounds, we have identified 19 drugs that block transforming growth factor beta (TGFβ)-induced EMT in normal murine mammary gland epithelial cells (NMuMG). The active compounds include inhibitors against TGFβ receptors (TGFBR), Rho-associated protein kinases (ROCK), myosin II, SRC kinase and uridine analogues. Among the EMT-repressing compounds, we identified a group of inhibitors targeting multiple receptor tyrosine kinases, and biochemical profiling of these multi-kinase inhibitors reveals TGFBR as a thus far unknown target of their inhibitory spectrum. These findings demonstrate the feasibility of a multi-parameter, high-content microscopy screen to identify modulators and druggable targets of EMT. Moreover, the newly discovered “off-target” effects of several receptor tyrosine kinase inhibitors have important consequences for in vitro and in vivo studies and might beneficially contribute to the therapeutic effects observed in vivo. PMID:27036020

  1. DNA-conjugated gold nanoparticles based colorimetric assay to assess helicase activity: a novel route to screen potential helicase inhibitors

    Science.gov (United States)

    Deka, Jashmini; Mojumdar, Aditya; Parisse, Pietro; Onesti, Silvia; Casalis, Loredana

    2017-01-01

    Helicase are essential enzymes which are widespread in all life-forms. Due to their central role in nucleic acid metabolism, they are emerging as important targets for anti-viral, antibacterial and anti-cancer drugs. The development of easy, cheap, fast and robust biochemical assays to measure helicase activity, overcoming the limitations of the current methods, is a pre-requisite for the discovery of helicase inhibitors through high-throughput screenings. We have developed a method which exploits the optical properties of DNA-conjugated gold nanoparticles (AuNP) and meets the required criteria. The method was tested with the catalytic domain of the human RecQ4 helicase and compared with a conventional FRET-based assay. The AuNP-based assay produced similar results but is simpler, more robust and cheaper than FRET. Therefore, our nanotechnology-based platform shows the potential to provide a useful alternative to the existing conventional methods for following helicase activity and to screen small-molecule libraries as potential helicase inhibitors. PMID:28287182

  2. RNA interference screening of interferon-stimulated genes with antiviral activities against classical swine fever virus using a reporter virus.

    Science.gov (United States)

    Wang, Xiao; Li, Yongfeng; Li, Lian-Feng; Shen, Liang; Zhang, Lingkai; Yu, Jiahui; Luo, Yuzi; Sun, Yuan; Li, Su; Qiu, Hua-Ji

    2016-04-01

    Classical swine fever (CSF) caused by classical swine fever virus (CSFV) is a highly contagious and often fatal disease of pigs, which leads to significant economic losses in many countries. Viral infection can induce the production of interferons (IFNs), giving rise to the transcription of hundreds of IFN-stimulated genes (ISGs) to exert antiviral effects. Although numerous ISGs have been identified to possess antiviral activities against different viruses, rare anti-CSFV ISGs have been reported to date. In this study, to screen anti-CSFV ISGs, twenty-one ISGs reported previously were individually knocked down using small interfering RNAs (siRNAs) followed by infection with a reporter CSFV expressing Renilla luciferase (Rluc). As a result, four novel anti-CSFV ISGs were identified, including natural-resistance-associated macrophage protein 1 (NRAMP1), cytosolic 5'-nucleotidase III A (NT5C3A), chemokine C-X-C motif ligand 10 (CXCL10), and 2'-5'-oligoadenylate synthetase 1 (OAS1), which were further verified to exhibit antiviral activities against wild-type CSFV. We conclude that the reporter virus is a useful tool for efficient screening anti-CSFV ISGs.

  3. Screening of marine fungus from Nanji Island and activity of their metabolites against pathogenic Vibrio from Pseudosciaena crocea

    Institute of Scientific and Technical Information of China (English)

    ZHAO Shujiang; LI Shuping; LIU Huihui; ZHAO Qian; WANG Jieyou; YAN Maocang

    2012-01-01

    Seventy-eight marine fungal strains were isolated from sediment samples collected offthe 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 Vibrio from Pseudosciaena crocea.Subsequent screening confirmed that nine strains produced antibacterial metabolites that had activity against one or several types of pathogenic Vibrio.Strain N J0104 had the widest antimicrobial spectrum and strong activity,particularly against Vibrio parahaemolyticus-MM0810072.A preliminary study of NJ0104antibacterial metabolites demonstrated that they had thermal stability up to 80℃,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.

  4. Use of activity-based probes to develop high throughput screening assays that can be performed in complex cell extracts.

    Directory of Open Access Journals (Sweden)

    Edgar Deu

    Full Text Available BACKGROUND: High throughput screening (HTS is one of the primary tools used to identify novel enzyme inhibitors. However, its applicability is generally restricted to targets that can either be expressed recombinantly or purified in large quantities. METHODOLOGY AND PRINCIPAL FINDINGS: Here, we described a method to use activity-based probes (ABPs to identify substrates that are sufficiently selective to allow HTS in complex biological samples. Because ABPs label their target enzymes through the formation of a permanent covalent bond, we can correlate labeling of target enzymes in a complex mixture with inhibition of turnover of a substrate in that same mixture. Thus, substrate specificity can be determined and substrates with sufficiently high selectivity for HTS can be identified. In this study, we demonstrate this method by using an ABP for dipeptidyl aminopeptidases to identify (Pro-Arg2-Rhodamine as a specific substrate for DPAP1 in Plasmodium falciparum lysates and Cathepsin C in rat liver extracts. We then used this substrate to develop highly sensitive HTS assays (Z'>0.8 that are suitable for use in screening large collections of small molecules (i.e >300,000 for inhibitors of these proteases. Finally, we demonstrate that it is possible to use broad-spectrum ABPs to identify target-specific substrates. CONCLUSIONS: We believe that this approach will have value for many enzymatic systems where access to large amounts of active enzyme is problematic.

  5. A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor.

    Science.gov (United States)

    Lotz-Jenne, Carina; Lüthi, Urs; Ackerknecht, Sabine; Lehembre, François; Fink, Tobias; Stritt, Manuel; Wirth, Matthias; Pavan, Simona; Bill, Ruben; Regenass, Urs; Christofori, Gerhard; Meyer-Schaller, Nathalie

    2016-05-03

    An epithelial to mesenchymal transition (EMT) enables epithelial tumor cells to break out of the primary tumor mass and to metastasize. Understanding the molecular mechanisms driving EMT in more detail will provide important tools to interfere with the metastatic process. To identify pharmacological modulators and druggable targets of EMT, we have established a novel multi-parameter, high-content, microscopy-based assay and screened chemical compounds with activities against known targets. Out of 3423 compounds, we have identified 19 drugs that block transforming growth factor beta (TGFβ)-induced EMT in normal murine mammary gland epithelial cells (NMuMG). The active compounds include inhibitors against TGFβ receptors (TGFBR), Rho-associated protein kinases (ROCK), myosin II, SRC kinase and uridine analogues. Among the EMT-repressing compounds, we identified a group of inhibitors targeting multiple receptor tyrosine kinases, and biochemical profiling of these multi-kinase inhibitors reveals TGFBR as a thus far unknown target of their inhibitory spectrum. These findings demonstrate the feasibility of a multi-parameter, high-content microscopy screen to identify modulators and druggable targets of EMT. Moreover, the newly discovered "off-target" effects of several receptor tyrosine kinase inhibitors have important consequences for in vitro and in vivo studies and might beneficially contribute to the therapeutic effects observed in vivo.

  6. 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.

  7. 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.

  8. Screening on the Pharmacodynemic Active Parts of Protecting Liver of Peristrope japonica (thunb.)Bremek

    Institute of Scientific and Technical Information of China (English)

    杨希雄; 皮慧芳; 张国欣; 庞雪冰; 吴继洲

    2004-01-01

    The pharmacodynamic active parts of protecting liver of Peristrope japonica (thunb.)Bremek were identified. Rat acute liver injury model was induced by D-galactosamine (D-GlaN).The active parts were identified on the whole extraction and 4 fractions. The results showed that the pharmacodynamic active parts of Peristrope japonica were the n-BuOH fraction.

  9. A Genetic Screen Identifies PITX1 as a Suppressor of RAS Activity and Tumorigenicity

    NARCIS (Netherlands)

    Kolfschoten, I.G.M.; Leeuwen, Bart van; Berns, K.; Mullenders, J.; Beijersbergen, R.L.; Bernards, R.A.; Voorhoeve, P.M.; Agami, R.

    2005-01-01

    Activating mutations of RAS frequently occur in subsets of human cancers, indicating that RAS activation is important for tumorigenesis. However, a large proportion of these cancers still retain wild-type RAS alleles, suggesting that either the RAS pathway is activated in a distinct manner or anothe

  10. Preliminary phytochemical screening and evaluation of antibacterial activity of Dichrocepala integrifolia (L.f O. kuntze

    Directory of Open Access Journals (Sweden)

    Tesfaye Mohammed

    2012-02-01

    Conclusion and Recommendation: In general the antimicrobial activity of the plant observed here support the tradition therapeutic claim of the society. Further study should be conducted in further evaluating its antimicrobial effectiveness and also purification of the active chemical constituents that could be responsible for its biological activity. [J Intercult Ethnopharmacol 2012; 1(1.000: 30-34

  11. Screening the antiangiogenic activity of medicinal plants grown and sold in Jordan.

    Science.gov (United States)

    Zihlif, Malek; Afifi, Fatma; Muhtaseb, Ruba; Al-Khatib, Sondos; Abaza, Ismail; Naffa, Randa

    2012-02-01

    Angiogenesis is essential for the growth, invasion, and metastasis of most solid tumors and has become a valuable pharmacological target for cancer prevention and treatment. This study was performed to assess the antiangiogenic activity of 31 medicinal plants grown and sold in Jordan. The antiangiogenic activity was assessed using the rat aortic ring assay. Out of 31 extracts, 15 extracts showed more than 50 % inhibition of the blood vessels outgrowth from the primary tissue explants (p = 0.000). Three of these 15 extracts showed a potential cytotoxic effect on normal fibroblast cells. Four extracts shared antiangiogenic and antiproliferative activity towards MCF7 breast cancer cell lines. Eight extracts demonstrated selective antiangiogenic activity. This is the first report demonstrating the potential antiangiogenic activity of Artemisia judaica, Aloysia citriodora, Salvia egyptiaca, and Calendula arvensis. Some extracts with antiangiogenic activity exhibited selectivity against the endothelial cells proliferation, demonstrating a direct inhibitory activity against the key step in tumor angiogenesis.

  12. Screening of 397 chemicals and development of a quantitative structure-activity relationship model for androgen receptor antagonism

    DEFF Research Database (Denmark)

    Vinggaard, Annemarie; Niemelä, Jay Russell; Wedebye, Eva Bay;

    2008-01-01

    We have screened 397 chemicals for human androgen receptor (AR) antagonism by a sensitive reporter gene assay to generate data for the development of a quantitative structure-activity relationship (QSAR) model. A total of 523 chemicals comprising data on 292 chemicals from our laboratory and data...... by the synthetic androgen R1881. The MultiCASE expert system was used to construct a QSAR model for AR antagonizing potential. A "5 Times, 2-Fold 50% Cross Validation" of the model showed a sensitivity of 64%, a specificity of 84%, and a concordance of 76%. Data for 102 chemicals were generated for an external...... validation of the model resulting in a sensitivity of 57%, a specificity of 98%, and a concordance of 92% of the model. The model was run on a set of 176103 chemicals, and 47% were within the domain of the model. Approximately 8% of chemicals was predicted active for AR antagonism. We conclude...

  13. Development and Application of a New Microarray- Based Method for High-Throughput Screening of Carbohydrate Active Enzymes

    DEFF Research Database (Denmark)

    Vidal Melgosa, Silvia

    biological roles in plants and in addition to biofuel production they are extensively used in other industrial processes including in detergents, textiles, paper and the food industry. A vast repertoire of CAZymes exists in nature but there is a growing disparity between our ability to putatively identify....... The applicability of the method to identify the substrate specificities of purified uncharacterised enzymes as well as for screening CAZyme activities in complex enzyme mixtures, such as crude culture broths and plant extracts, is shown by examples presented in this thesis. We envisage that the method......The effective and sustainable use of plant biomass for second generation biofuels is of vital importance for reducing dependence on fossil fuels. Carbohydrate-active enzymes (CAZymes) that degrade lignocellulosic plant cell wall material are an important part of this effort. CAZymes have multiple...

  14. A Class of High-affinity Bicyclooctane G551D-CFTR Activators Identified by High Throughput Screening

    Institute of Scientific and Technical Information of China (English)

    HE Cheng-yan; ZHAO Lu; LIU Yan-li; XU Li-na; SHANG De-jing; YANG Hong

    2004-01-01

    The glycine-to-aspartic acid missense mutation at the codon 551(G551D) of the cystic fibrosis transmembrane conductance regulator(CFTR) is one of the five most frequent cystic fibrosis(CF) mutations associated with a severe CF phenotype. To explore the feasibility of pharmacological correction of disrupted activation of CFTR chloride channel caused by G551D mutation, we developed a halide-sensitive fluorescence miniassay for G551D-CFTR in Fisher rat thyroid(FRT) epithelial cells for the discovery of novel activators of G551D-CFTR. A class of bicyclooctane small molecule compounds that efficiently stimulate G551D-CFTR chloride channel activity was identified by high throughput screening via the FRT cell-based assay. This class of compounds selectively activates G551D-CFTR with a high affinity, whereas little effect of the compounds on wildtype CFTR can be seen. The discovery of a class of bicyclooctane G551D-CFTR activators will permit the analysis of structure-activity relationship of the compounds to identify ideal leads for in vivo therapeutic studies.

  15. 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.

  16. Screening of Lactic Acid Bacteria with Antioxidant Activity%抗氧化活性乳酸菌的筛选

    Institute of Scientific and Technical Information of China (English)

    刘天祎; 潘道东

    2011-01-01

    In order to achieve lactic acid bacteria with high antioxidant activity,20 lactic acid bacterial strains were isolated from kimchi juice,goose intestines and chicken crop.Strains L8 and L17 with high antioxidant activity were picked out through preliminary screening based on DPPH and superoxide anion free radical scavenging activity and secondary screening based on total antioxidant capacity(T-AOC) and total superoxide dismutase(T-SOD) activity.Both strains were identified as Lactobacillus casei by carbohydrate fermentation,physiological and biochemical tests and 16S rDNA sequence analysis.%以获得高抗氧化活性乳酸菌菌株为目的,从泡菜汁、鹅肠、鸡嗉囊等材料中分离获得20株乳酸菌。以对DPPH自由基和O-2.的清除率为初筛指标,总抗氧化(T-AOC)能力和总超氧化物歧化酶(T-SOD)活力为复筛指标,筛选得到两株具有较高抗氧化活性的菌株L8和L17。利用糖发酵实验、生理生化实验和16S rDNA序列比对的方法对其进行鉴定,发现它们均为干酪乳杆菌。

  17. Screening active components from Yu-ping-feng-san for regulating initiative key factors in allergic sensitization.

    Science.gov (United States)

    Shen, Dandan; Xie, Xuejian; Zhu, Zhijie; Yu, Xi; Liu, Hailiang; Wang, Huizhu; Fan, Hongwei; Wang, Dawei; Jiang, Guorong; Hong, Min

    2014-01-01

    Yu-ping-feng-san (YPFS) is a Chinese medical formula that is used clinically for allergic diseases and characterized by reducing allergy relapse. Our previous studies demonstrated that YPFS efficiently inhibited T helper 2 cytokines in allergic inflammation. The underlying mechanisms of action of YPFS and its effective components remain unclear. In this study, it was shown that YPFS significantly inhibited production of thymic stromal lymphopoietin (TSLP), an epithelial cell-derived initiative factor in allergic inflammation, in vitro and in vivo. A method of human bronchial epithelial cell (16HBE) binding combined with HPLC-MS (named 16HBE-HPLC-MS) was established to explore potential active components of YPFS. The following five components bound to 16HBE cells: calycosin-7-glucoside, ononin, claycosin, sec-o-glucosylhamaudol and formononetin. Serum from YPFS-treated mice was analyzed and three major components were detected claycosin, formononetin and cimifugin. Among these, claycosin and formononetin were detected by 16HBE-HPLC-MS and in the serum of YPFS-treated mice. Claycosin and formononetin decreased the level of TSLP markedly at the initial stage of allergic inflammation in vivo. Nuclear factor (NF)-κB, a key transcription factor in TSLP production, was also inhibited by claycosin and formononetin, either in terms of transcriptional activation or its nuclear translocation in vitro. Allergic inflammation was reduced by claycosin and formononetin when they are administered only at the initial stage in a murine model of atopic contact dermatitis. Thus, epithelial cell binding combined with HPLC-MS is a valid method for screening active components from complex mixtures of Chinese medicine. It was demonstrated that the compounds screened from YPFS significantly attenuated allergic inflammation probably by reducing TSLP production via regulating NF-κB activation.

  18. Screening of twenty five plant extracts for larvicidal activity against Culex quinquefasciatus Say (Diptera:Culicidae)

    Institute of Scientific and Technical Information of China (English)

    Samuel Tennyson; K John Ravindran; S Arivoli

    2012-01-01

    Objective: To determine the larvicidal activity of twenty five plant extracts against Culex quinquefasciatus (Cx. quinquefasciatus). Methods: The larvicidal activity was determined against the third instar larvae of Cx. quinquefasciatus at 1 000 ppm concentration. Larval mortality was assessed after 24 and 48 h. Results: The hexane extracts of Cleistanthus collinus (C. collinus) and Murraya koeingii (M. koeingii) plants showed 100 percent mortality at 24 h bioassay followed by diethyl ether, dichloromethane and ethyl acetate extracts of C. collinus, Leucas aspera (L. aspera), Hydrocotyle javanica (H. javanica), M. koeingii, Sphaeranthus indicus (S. indicus) and Zanthoxylum limonella (Z. limonella) after 48 h exposure. Conclusions: The results indicate larvicidal activity against Cx. quinquefasciatus and further investigations are needed to elucidate this activity against a wide range of all stages of mosquito species and also the active ingredients of the extract responsible for larvicidal activity should be identified.

  19. 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

    2011-06-01

    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.

  20. 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.

  1. 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.

  2. Annotated compound data for modulators of detergent-solubilised or lipid-reconstituted respiratory type II NADH dehydrogenase activity obtained by compound library screening

    OpenAIRE

    Dunn, Elyse A.; Cook, Gregory M.; Adam Heikal

    2015-01-01

    The energy-generating membrane protein NADH dehydrogenase (NDH-2), a proposed antibacterial drug target (see “Inhibitors of type II NADH:menaquinone oxidoreductase represent a class of antitubercular drugs” Weinstein et al. 2005 [1]), was screened for modulators of activity in either detergent-solublised or lipid reconstituted (proteolipsome) form. Here we present an annotated list of compounds identified in a small-scale screen against NDH-2. The dataset contains information regarding the li...

  3. 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

  4. 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.

  5. 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.

  6. 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.

  7. Screening for antibacterial principle and activity of Aerva javanica (Burm .f) Juss. ex Schult.

    Institute of Scientific and Technical Information of China (English)

    P Srinivas; S Ram Reddy

    2012-01-01

    Objective: To investigate the antibacterial principle and activity of Aerva javanica, a medicinal plant. Methods: Crude extracts of different parts of Aerva javanica were made with hexane, chloroform and methanol. Phytochemical analysis of the crude extracts was done by following the standard methodology, and antibacterial activity was evaluated by inhibition zone and MIC values. Crude extracts were resolved through HPTLC and the antibacterial activity of the separated compounds was evaluated by bioautography. Results: The yields of crude extracts made from different plant parts varied both with plant part and solvent. Methanolic extracts of leaf and flower have shown a wide range of phytochemicals and more antibacterial activity. HPTLC separation of extracts coupled with bioautography studies revealed that apigenin followed by rutin and kaempferol has shown antibacterial activity against more number of bacteria. Conclusions:The present study supports the use of Aerva javanica in the traditional medicine, and it can be used against bacterial infections.

  8. 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.

  9. 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.

  10. Location performance objectives for the NNWSI area-to-location screening activity

    Energy Technology Data Exchange (ETDEWEB)

    Sinnock, S.; Fernandez, J.A.

    1984-01-01

    Fifty-four objectives were identified to guide the screening of the Nevada Research and Development Area of the Nevada Test Site for relatively favorable locations for the disposal of nuclear waste in a mined geologic repository. The objectives were organized as a hierarchy composed of 4 upper-level, 12 middle-level, and 38 lower-level objectives. The four upper-level objectives account for broad national goals to contain and isolate nuclear waste in an environmentally sound and economically acceptable manner. The middle-level objectives correspond to topical categories that logically relate the upper-level objectives to site-specific concerns such as seismicity, sensitive species, and flooding hazards (represented by the lower-level objectives). The relative merits of alternative locations were compared by an application of decision analysis based on standard utility theory. The relative favorabilities of pertinent physical conditions at each alternative location were weighted in relation to the importance of objectives, and summed to produce maps indicating the most and the least favorable locations. Descriptions of the objectives were organized by the hierarchical format; they detail the applicability of each objective to geologic repository siting, previously published siting criteria corresponding to each objective, and the rationale for the weight assigned to each objective, and the pertinent attributes for evaluating locations with respect to each objective. 51 references, 47 figures, 4 tables.

  11. Screening of marine bacteria with bacteriocin-like activities and probiotic potential for ornate spiny lobster (Panulirus ornatus) juveniles.

    Science.gov (United States)

    Nguyen, Van Duy; Pham, Thu Thuy; Nguyen, Thi Hai Thanh; Nguyen, Thi Thanh Xuan; Hoj, Lone

    2014-09-01

    Bacteriocins are ribosomally synthesized antimicrobial peptides, which have been found in diverse bacterial species of terrestrial origins and some from the sea. New bacteriocins with new characteristics, new origins and new applications are likely still awaiting discovery. The present study screened bacteria isolated from marine animals of interest to the aquaculture industry for antimicrobial and bacteriocin-like activities in order to uncover biodiversity of bacteriocin producers, and explore the potential application in aquaculture. In total, 24 of 100 screened isolates showed antimicrobial activities and 7 of these exerted bacteriocin-like activities. Sequencing of 16S rRNA genes identified the isolates as members of the six genera Proteus, Providencia, Klebsiella, Alcaligenes, Bacillus and Enterococcus. In some cases, further analysis of housekeeping genes, rpoB for Proteus and recA for Klebsiella, as well as biochemical tests was necessary for identification to species level, and some of the Proteus isolates may represent novel species. The seven bacteriocinogenic isolates showed a wide antimicrobial spectrum against foodborne and animal pathogens, which opens the way to their potential use as marine drugs and probiotics in food, aquaculture, livestock and clinical settings. As a case study, the protective effect of shortlisted bacteriocinogenic isolates were tested in aquaculture-raised spiny lobster (Panulirus ornatus) juveniles. A single-strain (Bacillus pumilus B3.10.2B) and a three-strain (B. pumilus B3.10.2B, Bacillus cereus D9, Lactobacillus plantarum T13) probiotic preparation were added to the feed of Panulirus ornatus juveniles, which were subsequently challenged with the pathogen Vibrio owensii DY05. Juveniles in the probiotic treatments displayed increased growth and reduced feed conversion rates after 60 days, and increased survival rate after pathogen challenge relative to the control. This study represents the first evidence of bacteriocin

  12. Antimicrobial peptides: mediators of innate immunity as templates for the development of novel anti-infective and immune therapeutics.

    Science.gov (United States)

    Hiemstra, P S; Fernie-King, B A; McMichael, J; Lachmann, P J; Sallenave, J-M

    2004-01-01

    Antimicrobial molecules are ancient and essential small cationic molecules of the host defence system which are found in a wide variety of species. They display antimicrobial activity against a wide range of bacteria, fungi and viruses, an activity that has been mostly attributed to the disruption of microbial membranes. In this article, we will review the "classical" functions of 3 classes of antimicrobial molecules, namely defensins, cathelicidins, and the four-disulfide core proteins secretory leukocyte proteinase inhibitor (SLPI) and elafin. In addition to the study of their expression in a variety of cell types and the regulation of their production, we will also describe novel properties of these molecules that have been highlighted by recent studies. These include their ability to chemoattract a variety of inflammatory, immune and other cell types (neutrophils, macrophages, monocytes, lymphocytes, mast cells, epithelial cells) in vitro and in vivo. In addition, we will discuss the potential use of these newly discovered properties for therapeutic or vaccination purposes, using protein- or gene-transfer based methodologies. Finally, we will examine in an extensive fashion the strategies used by microorganisms to circumvent and subvert host defence mechanisms, such as the modifications of cell membranes and walls, the secretion of inactivating proteins and proteases and the down-regulation of expression of antimicrobial molecules. Increased understanding of the mechanisms used by both the host and the microbes to 'win the battle' may ultimately lead to new therapeutic strategies aimed to treat infectious diseases.

  13. Association between the Family Nutrition and Physical Activity screening tool and cardiovascular disease risk factors in 10-year old children

    Science.gov (United States)

    Yee, Kimbo Edward

    Purpose. To examine the association of the Family Nutrition and Physical Activity (FNPA) screening tool, a behaviorally based screening tool designed to assess the obesogenic family environment and behaviors, with cardiovascular disease (CVD) risk factors in 10-year old children. Methods. One hundred nineteen children were assessed for body mass index (BMI), percent body fat (%BF), waist circumference (WC), total cholesterol, HDL-cholesterol, and resting blood pressure. A continuous CVD risk score was created using total cholesterol to HDL-cholesterol ratio (TC:HDL), mean arterial pressure (MAP), and WC. The FNPA survey was completed by parents. The associations between the FNPA score and individual CVD risk factors and the continuous CVD risk score were examined using correlation analyses. Results. Approximately 35% of the sample were overweight (19%) or obese (16%). The mean FNPA score was 24.6 +/- 2.5 (range 18 to 29). Significant correlations were found between the FNPA score and WC (r = -.35, prisk score (r = -.22, p = .02). No significant association was found between the FNPA score and TC:HDL (r=0.10, p=0.88) or MAP (r=-0.12, p=0.20). Conclusion. Children from a high-risk, obesogenic family environment as indicated with a lower FNPA score have a higher CVD risk factor profile than children from a low-risk family environment.

  14. Efficacy of Allium cepa test system for screening cytotoxicity and genotoxicity of industrial effluents originated from different industrial activities.

    Science.gov (United States)

    Pathiratne, Asoka; Hemachandra, Chamini K; De Silva, Nimal

    2015-12-01

    Efficacy of Allium cepa test system for screening cytotoxicity and genotoxicity of treated effluents originated from four types of industrial activities (two textile industries, three rubber based industries, two common treatment plants of industrial zones, and two water treatment plants) was assessed. Physico-chemical parameters including the heavy metal/metalloid levels of the effluents varied depending on the industry profile, but most of the measured parameters in the effluents were within the specified tolerance limits of Sri Lankan environmental regulations for discharge of industrial effluents into inland surface waters. In the A. cepa test system, the undiluted effluents induced statistically significant root growth retardation, mitosis depression, and chromosomal aberrations in root meristematic cells in most cases in comparison to the dilution water and upstream water signifying effluent induced cytotoxicity and genotoxicity. Ethyl methane sulphonate (a mutagen, positive control) and all the effluents under 1:8 dilution significantly induced total chromosomal aberrations in root meristematic cells in comparison to the dilution water and upstream water indicating inadequacy of expected 1:8 dilutions in the receiving waters for curtailing genotoxic impacts. The results support the use of a practically feasible A. cepa test system for rapid screening of cytotoxicity and genotoxicity of diverse industrial effluents discharging into inland surface waters.

  15. Photocatalytic decolouration of Orange II by ZnO active layers screen-printed on ceramic tiles.

    Science.gov (United States)

    Marto, J; São Marcos, P; Trindade, T; Labrincha, J A

    2009-04-15

    In this work ZnO layers have been deposited by screen-printing in common ceramic tiles. These layers were characterized and tested for the photocatalytic degradation of the organic dye Orange II in aqueous solutions, using a batch photoreactor either under visible light provided by a Philips ML-160 W lamp or under direct exposure to sunlight. For sake of comparison, ZnO suspensions have also been evaluated for similar reacting conditions. The influence of experimental parameters such as (i) firing temperature of the printed layer; (ii) layer thickness; and (iii) operation time have been investigated. Screen-printed ZnO layers obtained in optimal processing conditions showed photocatalytic activity comparable to aqueous ZnO suspensions. The maximal attenuation degree is over 70% and decolourisation rate, assuming that reaction kinetics follows a pseudo-first order rate law, is over 0.015 min(-1). Thus these ZnO-layered ceramic tiles can be regarded as an alternative to photocatalytic suspensions of the same material with the advantage of avoiding the removal of the photocatalyst.

  16. Defining RNA motif-aminoglycoside interactions via two-dimensional combinatorial screening and structure-activity relationships through sequencing.

    Science.gov (United States)

    Velagapudi, Sai Pradeep; Disney, Matthew D

    2013-10-15

    RNA is an extremely important target for the development of chemical probes of function or small molecule therapeutics. Aminoglycosides are the most well studied class of small molecules to target RNA. However, the RNA motifs outside of the bacterial rRNA A-site that are likely to be bound by these compounds in biological systems is largely unknown. If such information were known, it could allow for aminoglycosides to be exploited to target other RNAs and, in addition, could provide invaluable insights into potential bystander targets of these clinically used drugs. We utilized two-dimensional combinatorial screening (2DCS), a library-versus-library screening approach, to select the motifs displayed in a 3×3 nucleotide internal loop library and in a 6-nucleotide hairpin library that bind with high affinity and selectivity to six aminoglycoside derivatives. The selected RNA motifs were then analyzed using structure-activity relationships through sequencing (StARTS), a statistical approach that defines the privileged RNA motif space that binds a small molecule. StARTS allowed for the facile annotation of the selected RNA motif-aminoglycoside interactions in terms of affinity and selectivity. The interactions selected by 2DCS generally have nanomolar affinities, which is higher affinity than the binding of aminoglycosides to a mimic of their therapeutic target, the bacterial rRNA A-site.

  17. Screening of Dengue virus antiviral activity of marine seaweeds by an in situ enzyme-linked immunosorbent assay.

    Directory of Open Access Journals (Sweden)

    Andrea Cristine Koishi

    Full Text Available Dengue is a significant public health problem worldwide. Despite the important social and clinical impact, there is no vaccine or specific antiviral therapy for prevention and treatment of dengue virus (DENV infection. Considering the above, drug discovery research for dengue is of utmost importance; in addition natural marine products provide diverse and novel chemical structures with potent biological activities that must be evaluated. In this study we propose a target-free approach for dengue drug discovery based on a novel, rapid, and economic in situ enzyme-linked immunosorbent assay and the screening of a panel of marine seaweed extracts. The in situ ELISA was standardized and validated for Huh7.5 cell line infected with all four serotypes of DENV, among them clinical isolates and a laboratory strain. Statistical analysis showed an average S/B of 7.2 and Z-factor of 0.62, demonstrating assay consistency and reliability. A panel of fifteen seaweed extracts was then screened at the maximum non-toxic dose previously determined by the MTT and Neutral Red cytotoxic assays. Eight seaweed extracts were able to reduce DENV infection of at least one serotype tested. Four extracts (Phaeophyta: Canistrocarpus cervicornis, Padina gymnospora; Rhodophyta: Palisada perforate; Chlorophyta: Caulerpa racemosa were chosen for further evaluation, and time of addition studies point that they might act at an early stage of the viral infection cycle, such as binding or internalization.

  18. Isolation, Identification And Screening Antibacterial Activity from Marine Sponge-Associated Fungi Against Multidrug-Resistant (MDR) Escherichia coli

    Science.gov (United States)

    Triandala Sibero, Mada; Sabdaningsih, Aninditia; Cristianawati, Olvi; Nuryadi, Handung; Karna Radjasa, Ocky; Sabdono, Agus; Trianto, Agus

    2017-02-01

    Irrational used of antibiotic in several decades ago causing resistant in bacteria and decreasing the cure rate of infectious diseases. Multidrug-resistant (MDR) Escherichia coli is known to cause various of infectious diseases such as urinary tract infection, nosocomial bloodstream infection, meningitis, bacteraemia, and gastrointestinal disease. Marine sponge-associated fungi have potential as source of new compound to combat MDR E. coli. The aims of this research were to isolate marine sponge-assosiated fungi, to screen potential fungi against MDR E. coli, to identify the potential fungi and its host sponge. There were 29 marine sponge-associated fungi successfully isolated from 9 sponges. Among 29 sponge-associated fungi screened, there were 7 isolates showed antibacterial activity against MDR E. coli. The best inhibition zone produced by MPS 14.1/MT 02 and MPS 14.3/MT 04 from sponge PP.SP.16.14. According to fungi identification result fungus MPS 14.1/MT 02 was identified as Trichoderma asperellum while MPS 14.3/MT 04 was identified as Trichoderma reesei. Sponge identification leaded the PP.SP.16.14 as Cinachyrella sp.

  19. High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses.

    Directory of Open Access Journals (Sweden)

    Deu John M Cruz

    Full Text Available Dengue virus is a mosquito-borne flavivirus that has a large impact in global health. It is considered as one of the medically important arboviruses, and developing a preventive or therapeutic solution remains a top priority in the medical and scientific community. Drug discovery programs for potential dengue antivirals have increased dramatically over the last decade, largely in part to the introduction of high-throughput assays. In this study, we have developed an image-based dengue high-throughput/high-content assay (HT/HCA using an innovative computer vision approach to screen a kinase-focused library for anti-dengue compounds. Using this dengue HT/HCA, we identified a group of compounds with a 4-(1-aminoethyl-N-methylthiazol-2-amine as a common core structure that inhibits dengue viral infection in a human liver-derived cell line (Huh-7.5 cells. Compounds CND1201, CND1203 and CND1243 exhibited strong antiviral activities against all four dengue serotypes. Plaque reduction and time-of-addition assays suggests that these compounds interfere with the late stage of viral infection cycle. These findings demonstrate that our image-based dengue HT/HCA is a reliable tool that can be used to screen various chemical libraries for potential dengue antiviral candidates.

  20. Screening of biological activities of Polygonum maritimum L. from Algerian coast

    Institute of Scientific and Technical Information of China (English)

    Imad Abdelhamid El-Haci; Fawzia Atik Bekkara; Wissame Mazari; Fayal Hassani; Mohamed Amine Didi

    2013-01-01

    Objective: To investigate the antioxidant and the antibacterial activities of crude extract from aerial part of Polygonum maritimum L. (Polygonaceae) (P. maritimum) and to find new actives biomolecules. Methods:The whole plant was collected from the Rechgoune coast (West of Algeria), and methanolic crude extract of aerial parts of P. maritimum (PMCE) was prepared. The extract was tested against different bacterial strain and tested for his ability to neutralize free radical (DPPH) and to scavenge the H2O2. Results:PMCE had a very high content of total phenol, which was (352.49±18.03) mg/g dry weight,expressed as gallic acid equivalent. PMCE exhibited excellent antioxidant activity, as measured using DPPH and H2O2 scavenging assays. It also showed a high antibacterial activity against gram-positive bacterial strains: Bacillus cereus, Bacillus subtilis and Staphylococcus aureus with an highest MIC of 120 µg/mL. Conclusions: The antioxidant and antibacterial activity of the PMCE is probably due to phenolic compounds present in the extract. The contemporary presence of antioxidant and antibacterial activities in the PMCE suggests that this plant may be a source of bioactive substances with multifaceted activity.

  1. Screening of alkaloidal fraction of Conium maculatum L. aerial parts for analgesic and antiinflammatory activity

    Directory of Open Access Journals (Sweden)

    Reecha Madaan

    2012-01-01

    Full Text Available Conium maculatum Linn. (Umbelliferae has been traditionally used in the treatment of spasmodic disorders, and to relieve nervous excitation, rheumatic pains in the old and feeble, pain in stomach, pain of gastric ulcer, nervousness and restlessness. Alkaloids have long been considered as bioactive group of constituents present in C. maculatum. Despite a long tradition of use, C. maculatum has not been evaluated pharmacologically to validate its traditional claims for analgesic and antiinflammatory activities. Thus, the present investigations were undertaken with an objective to evaluate alkaloidal fraction of C. maculatum aerial parts for analgesic and antiinflammatory activities. Test doses (100 or 200 mg/kg, p.o. of alkaloidal fraction were evaluated for analgesic activity using tail flick test and antiinflammatory activity using carrageenan-induced paw oedema test in rats. Morphine (5 mg/kg, p.o. and indomethacin (5 mg/kg, p.o. were used as standard analgesic and antiinflammatory drugs, respectively. Alkaloidal fraction of the plant exhibited significant analgesic activity at a dose of 200 mg/kg as it showed significant increase in tail flicking reaction time with respect to the control during 2 h intervals of observation. It also exhibited significant antiinflammatory activity at a dose of 200 mg/kg as it inhibited paw oedema in rats to 71% and reduced the paw volume one-fourth to the control during 1 st h of the study. The present investigations suggest that alkaloids are responsible for analgesic and antiinflammatory activities of C. maculatum.

  2. In vitro screening of 1-aryl-6-hydroxy-1,2,3,4-tetrahydroisoquinolines: structure related activity against pathogenic bacteria

    Institute of Scientific and Technical Information of China (English)

    Moses; Njutain; Ngemenya; Joelle; Ngo; Hanna; Julios; Armand; Komtchou; Simon; Mbua; Ngale; Efange

    2015-01-01

    Objective: To evaluate the antibacterial activity of ten synthetic tetrahydroisoquinolines against eight bacterial strains. Methods: The ten tetrahydroisoquinolines synthesized via base-catalyzed Pictet-Spengler cyclization were screened against a total of eight bacterial strains comprising control and pathogenic strains by the disc diffusion and micro-dilution methods. The most active compound was then assessed for cytotoxicity on human lymphocytes. Results: Six of the tetrahydroisoquinolines showed broad spectrum bacteriostatic activity. The zones of inhibition produced ranged from 7 to 23 mm for 200 μg per disc. The presence of a lipophilic substituent at the para position of the pendant phenyl group conferred the highest antibacterial activity. Compound 2 [1-(3,4-chlorophenyl)-6-hydroxy-1,2,3,4-tetrahydroisoquinoline] was the most active and produced zones ranging from 9 to 20 mm against all eight bacterial strains. Compound 2 also showed the lowest minimum inhibitory concentration of 100 μg/mL against Escherichia coli ATCC11775 and the lowest minimum bactericidal concentration of 800 μg/mL against pathogenic Salmonella typhimurium. Overall, compound 2 was the most active with bacteriostatic and bactericidal activity against three and four bacterial strains respectively. A 50% cytotoxic concentration of 98.2 μg/mL was recorded for compound 2 indicating a low risk of toxicity. Conclusions: The 1-aryl-1,2,3,4-tetrahydroisoquinolines display structure-related antibacterial activity and further chemical exploration of the tetrahydroisoquinoline scaf old may yield more potent non-toxic derivatives for development into new antibacterials.

  3. Pharmacological screening of Hypericum androsaemum extracts for antioxidant, anti-lipid peroxidation, antiglycation and cytotoxicity activity.

    Science.gov (United States)

    Saddiqe, Zeb; Maimoona, Alya; Abbas, Ghulam; Naeem, Ismat; Shahzad, Muhammad

    2016-03-01

    Oxidative stress and glycation processes have a combined effect on diabetes related complications. Crude plant extracts and plant derived compounds possessing both antiglycation and antioxidant activities have a high therapeutic potential for treating these complications. Antioxidant, antiglycation, anti-lipid per oxidation and cytotoxic activities of crude methanol extract and solvent fractions of Hypericum androsaemum L. (Hypericaceae) were evaluated and correlated with total content of phenolics and flavonoids. Significant radical scavenging activity was observed for the methanol extract against 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical used as a basis for antioxidant activity with IC50 value of 92.70±2.85 μg mL(-1) (96.20±2.34% inhibition at 500 μg mL(-1)). In case of anion scavenging activity the results were not very significant (33.20±1.22% inhibition at 500 μg mL(-1)). Anti-lipid per oxidation activity was highest for n-hexane fraction (67.83±1.33% inhibition at 500 μg mL(-1)) while the ethyl acetate fraction had the highest antiglycation activity (62.77±2.54% inhibition at 500 μg mL(-1)). Statistically significant correlation was determined for antioxidant and antiglycation activity and phenolic and flavonoid contents. In cytotoxicity assay all the extracts had IC50 values >30 μg mL(-1) as compared to the standard cycloheximide (IC50 value 0.084±0.1 μg mL(-1)). The polar extracts of H. androsaemum can be a good source of non-toxic compounds with antioxidant, anti-lipid per oxidation and antiglycation activities.

  4. 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

  5. Screening of radical scavenging activity of some medicinal and aromatic plant extracts

    NARCIS (Netherlands)

    Miliauskas, G.; Venskutonis, R.P.; Beek, van T.A.

    2004-01-01

    Extracts of 12 medicinal and aromatic plants were investigated for their radical scavenging activity using DPPH and ABTS assays: Salvia sclarea, Salvia glutinosa, Salvia pratensis, Lavandula angustifolia, Calendula officinalis, Matricaria recutita, Echinacea purpurea, Rhaponticum carthamoides, Jugla

  6. Screening of antibacterial activity of raspberry (Rubus idaeus L. fruit and pomace extracts

    Directory of Open Access Journals (Sweden)

    Velićanski Aleksandra S.

    2012-01-01

    Full Text Available Antibacterial activity of fruit and pomace extracts (concentration 50 mg/ml of two raspberry (Rubus idaeus L. cultivars (Meeker and Willamette was tested against selected Gram-positive and Gram-negative bacteria (reference and wild strains. Disc diffusion method with 15 μl of extracts and agar-well diffusion method with 50 and 100 μl were used. Antibiotic (cefotaxime/clavulanic acid was used as a control. Both raspberry fruit extracts showed the strongest antibacterial activity against Pseudomonas aeruginosa (wild strain and Bacillus cereus, where the largest clear zones (without growth appeared. Escherichia coli was the most resistant strain, with only zone of reduced growth. The highest antibacterial activity of pomace extracts was against Staphylococcus aureus and Staphylococcus saprophyticus. There were no differences in the antibacterial activity between cultivars for both fruit and pomace extracts. [Projekat Ministarstva nauke Republike Srbije, br. TR 31044

  7. PHYTOCHEMICAL SCREENING AND ANTIBACTERIAL ACTIVITY FROM NERIUM OLEANDER AND EVALUVATE THEIR PLANT MEDIATED NANOPARTICLE SYNTHESIS

    Directory of Open Access Journals (Sweden)

    R.S. Suganya

    2012-05-01

    Full Text Available Phytochemical and antibacterial activity of essential oils obtained from Nerium oleander leaf with the help of three different extracts like ethanol, Methanol, and acetone. In this aqueous leaf extracts confirms the presence of various phytochemicals. To evaluate the antibacterial activities of these aqueous extracts were determined by disc diffusion method. From these three extracts methanol shows strong antibacterial effect on Klebsiella, Pseudomonas, Alkaligenes except Acinetobacter. None of the leaf extracts show no more activity in Acinetobacter. Biologically synthesized nanoparticles have been widely used in the field of medicine. Shade dried leaves of Nerium oleander was used for the synthesis of silver nanoparticles. UV- Visible spectroscopy studies were carried out to assess the formation of Ag nanoparticles. Scanning electron microscope (SEM was used to characterize the Ag nanoparticle. To compare the antimicrobial activity of silver nanoparticles with the different leaf extracts.

  8. Screening Approach to the Activation of Soil and Contamination of Groundwater at Linear Proton Accelerator Sites

    CERN Document Server

    Otto, Thomas

    The activation of soil and the contamination of groundwater at proton accelerator sites with the radionuclides 3H and 22Na are estimated with a Monte-Carlo calculation and a conservative soil- and ground water model. The obtained radionuclide concentrations show that the underground environment of future accelerators must be adequately protected against a migration of activation products. This study is of particular importance for the proton driver accelerator in the planned EURISOL facility.

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

    DEFF Research Database (Denmark)

    Lei, Tian; Engelbrecht, Kurt; Nielsen, K. K.;

    2011-01-01

    In active magnetic regeneration (AMR) systems, not only the magnetocaloric properties of materials, but also the regenerator geometry plays an important role in the system performance. Packed sphere regenerators are often employed in existing prototypes, however, the characteristics such as relat......In active magnetic regeneration (AMR) systems, not only the magnetocaloric properties of materials, but also the regenerator geometry plays an important role in the system performance. Packed sphere regenerators are often employed in existing prototypes, however, the characteristics...

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

    DEFF Research Database (Denmark)

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

    2014-01-01

    In active magnetic regeneration (AMR) systems, not only the magnetocaloric properties of materials, but also the regenerator geometry plays an important role in the system performance. Packed sphere regenerators are often employed in existing prototypes, however, the characteristics such as relat......In active magnetic regeneration (AMR) systems, not only the magnetocaloric properties of materials, but also the regenerator geometry plays an important role in the system performance. Packed sphere regenerators are often employed in existing prototypes, however, the characteristics...

  11. PHYTOCHEMICAL SCREENING AND IN VITRO ANTIOXIDANT ACTIVITY OF AQUEOUS AND HYDROALCOHOLIC EXTRACT OF BACOPA MONNIERI LINN.

    Directory of Open Access Journals (Sweden)

    Monic Shah et al

    2012-09-01

    Full Text Available The present study was undertaken to investigate in-vitro antioxidant activity of aqueous and hydroalcoholic extract of whole plant of Bacopa monnieri Linn. Family- Scrophularaceae. The total Phenolic content was determined using folin ciocalteau method while the total flavonoid content was determined using aluminium chloride method. In vitro antioxidant activity was evaluated using the Reducing power assay, Hydrogen peroxide scavenging assay, nitric oxide scavenging activity, superoxide scavenging activity and hydroxyl radical scavenging activity. The hydroalcoholic extract had more phenol concentration (116.1 mg/g of extract when compared to aqueous extract (58 mg/g of extract. The flavonoid content was more in hydroalcoholic extract (242.6 mg/g of extract when compared to that of aqueous extract (202.8 mg/g of extract. The reducing power and hydrogen peroxide scavenging of the extract was found to be concentration dependent. The nitric oxide scavenging activity, superoxide scavenging activity and Hydroxyl radical scavenging activity was also concentration dependent with IC50 value being 254.70 µg/ml , 934.06 µg/ml and 510.60 µg/ml respectively for Aqueous extract and 169.22 µg/ml, 495.83 µg/ml, 488 µg/ml respectively for hydroalcoholic extract. The order of the antioxidant potency of the whole plant extract is Hydroalcoholic >> aqueous. The results clearly indicate that aqueous and hydroalcoholic extract of Bacopa monnieri has anti oxidant property which may be due to the presence of phenols and flavonoids.

  12. Screening of immunomodulatory activity of total and protein extracts of some Moroccan medicinal plants.

    Science.gov (United States)

    Daoudi, Abdeljlil; Aarab, Lotfi; Abdel-Sattar, Essam

    2013-04-01

    Herbal and traditional medicines are being widely used in practice in many countries for their benefits of treating different ailments. A large number of plants in Morocco were used in folk medicine to treat immune-related disorders. The objective of this study is to evaluate the immunomodulatory activity of protein extracts (PEs) of 14 Moroccan medicinal plants. This activity was tested on the proliferation of immune cells. The prepared total and PEs of the plant samples were tested using MTT (3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide) assay on the splenocytes with or without stimulation by concanavalin-A (Con-A), a mitogenic agent used as positive control. The results of this study indicated different activity spectra. Three groups of activities were observed. The first group represented by Citrullus colocynthis, Urtica dioica, Elettaria cardamomum, Capparis spinosa and Piper cubeba showed a significant immunosuppressive activity. The second group that showed a significant immunostimulatory activity was represented by Aristolochia longa, Datura stramonium, Marrubium vulgare, Sinapis nigra, Delphynium staphysagria, Lepidium sativum, Ammi visnaga and Tetraclinis articulata. The rest of the plant extracts did not alter the proliferation induced by Con-A. This result was more important for the PE than for the total extract. In conclusion, this study revealed an interesting immunomodulating action of certain PEs, which could explain their traditional use. The results of this study may also have implications in therapeutic treatment of infections, such as prophylactic and adjuvant with cancer chemotherapy.

  13. An in vitro screening with emerging contaminants reveals inhibition of carboxylesterase activity in aquatic organisms.

    Science.gov (United States)

    Solé, Montserrat; Sanchez-Hernandez, Juan C

    2015-12-01

    Pharmaceuticals and personal care products (PPCPs) form part of the new generation of pollutants present in many freshwater and marine ecosystems. Although environmental concentrations of these bioactive substances are low, they cause sublethal effects (e.g., enzyme inhibition) in non-target organisms. However, little is known on metabolism of PPCPs by non-mammal species. Herein, an in vitro enzyme trial was performed to explore sensitivity of carboxylesterase (CE) activity of aquatic organisms to fourteen PPCPs. The esterase activity was determined in the liver of Mediterranean freshwater fish (Barbus meridionalis and Squalius laietanus), coastal marine fish (Dicentrarchus labrax and Solea solea), middle-slope fish (Trachyrhynchus scabrus), deep-sea fish (Alepocephalus rostratus and Cataetix laticeps), and in the digestive gland of a decapod crustacean (Aristeus antennatus). Results showed that 100μM of the lipid regulators simvastatin and fenofibrate significantly inhibited (30-80% of controls) the CE activity of all target species. Among the personal care products, nonylphenol and triclosan were strong esterase inhibitors in most species (36-68% of controls). Comparison with literature data suggests that fish CE activity is as sensitive to inhibition by some PPCPs as that of mammals, although their basal activity levels are lower than in mammals. Pending further studies on the interaction between PPCPs and CE activity, we postulate that this enzyme may act as a molecular sink for certain PPCPs in a comparable way than that described for the organophosphorus pesticides.

  14. Preliminary screening of Cuscuta reflexa stems for Anti inflammatory and cytotoxic activity

    Institute of Scientific and Technical Information of China (English)

    Pavan Bhausaheb Udavant; Suggala Venkata Satyanarayana; Chandrashekhar Devidas Upasani

    2012-01-01

    Objective: Evaluation of preliminary antiinflammatory and cytotoxic activities of a parasitic plant Cuscuta reflexa. Methods: Human red blood stabilizing activity was used for the evaluation of in vitro antiinflammatory activity and Brine shrimp lethality assay was used to assess the cytotoxic potential of extract of stems of Cuscuta reflexa. Results: Methanolic extract and Ethyl acetate fraction of methanolic extract of Cuscuta reflexa (MECR & EAMECR resp.) were found to have significant antiinflammatory and cytotoxic activity with inhibitory concentration IC50%values 277.83 μg/ml & 214.94 μg/ml in HRBC stabitlity assay[table 01], and lethal concentration LC50% 257.73 μg/ml 184.86 μg/ml in BSLA respectively[table 02]. Conclusions: Amongst various extracts evaluated for cytotoxicity and antiinflammatory activities, methanolic extract of Cuscutareflexa (MECR) and its ethyl acetate soluble fraction (EAMECR) show significant cytotoxic as well as antiinflammatory activities which may be due to the presence of phenols, polyphenols and flavonoids.

  15. Extraction of flavonoids from Tagetes patula: process optimization and screening for biological activity

    Directory of Open Access Journals (Sweden)

    Vanessa M. Munhoz

    2014-10-01

    Full Text Available The flowers of Tagetes patula L., Asteraceae, commonly known as French marigold, are used in folk medicine as an antiseptic, diuretic, blood purifier and insect repellent. This study was conducted to optimize the extraction process through the biomonitoring of flavonoids, using a statistical mixture simplex-centroid design, to evaluate the effect of the solvents water, ethanol and acetone, as well as mixtures of these solvents, assessed by the total flavonoid content. The extracts were tested for dry residue, radical scavenging activity, chromatographic profile, and larvicidal activity. The acetone extract had the highest total flavonoid content, 25.13 ± 1.02% (4.07%; and the best radical scavenging activity, with IC50 of 15.74 μg/ml ± 1.09 (6.92%, but with lower dry residue, 6.62 ± 1.33% (20.10%. The water extracts showed higher levels of dry residue, but lower total flavonoid content and radical scavenging activity than the acetone extract. The positive correlation between the total flavonoid content and radical scavenging activity of the extracts showed that flavonoids contribute significantly to the antioxidant capacity. The statistical mixture design allowed us to optimize the extraction of flavonoids from flowers of T. patula, with acetone as the best extraction solvent. Preliminary studies on the biological activity of the optimized extracts demonstrated a larvicidal effect of the acetone extract on Aedes aegypti mosquitoes.

  16. Screening of Asteraceae (Compositae Plant Extracts for Larvicidal Activity against Aedes fluviatilis (Diptera: Culicidae

    Directory of Open Access Journals (Sweden)

    Macêdo Maria E

    1997-01-01

    Full Text Available Ethanol extracts of 83 plants species belonging to the Asteraceae (Compositae family, collected in the State of Minas Gerais, Brazil, were tested for larvicidal activity against the mosquito Aedes fluviatilis - Diptera: Culicidae. The extract from Tagetes minuta was the most active with a LC90 of 1.5 mg/l and LC50 of 1.0 mg/l. This plant has been the object of several studies by other groups and its active components have already been identified as thiophene derivatives, a class of compounds present in many Asteraceae species. The extract of Eclipta paniculata was also significantly active, with a LC90 of 17.2 mg/l and LC50 of 3.3 mg/l and no previous studies on its larvicidal activity or chemical composition could be found in the literature. Extracts of Achryrocline satureoides, Gnaphalium spicatum, Senecio brasiliensis, Trixis vauthieri, Tagetes patula and Vernonia ammophila were less active, killing more than 50% of the larvae only at the higher dose tested (100 mg/l.

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

    NARCIS (Netherlands)

    L. Veldhuis (Lydian); A. van Grieken (Amy); C.M. Renders (Carry); R.A. Hirasing (Remy); H. Raat (Hein)

    2014-01-01

    textabstractIntroduction: The global increase in childhood overweight and obesity has been ascribed partly to increases in children's screen time. Parents have a large influence on their children's screen time. Studies investigating parenting and early childhood screen time are limited. In this stud

  18. Screening of bisphenol A, triclosan and paraben analogues as modulators of the glucocorticoid and androgen receptor activities.

    Science.gov (United States)

    Kolšek, Katra; Gobec, Martina; Mlinarič Raščan, Irena; Sollner Dolenc, Marija

    2015-02-01

    A homeostasis of the glucocorticoid and androgen endocrine system is essential to human health. Their disturbance can lead to various diseases, for example cardiovascular, inflammatory and autoimmune diseases, infertility, cancer. Fifteen widely used industrial chemicals that disrupt endocrine activity were selected for evaluation of potential (anti)glucocorticoid and (anti)androgenic activities. The human breast carcinoma MDA-kb2 cell line was utilized for reporter gene assays, since it expresses both the androgen and the glucocorticoid-responsive reporter. Two new antiandrogens, 4,4'-sulfonylbis(2-methylphenol) (dBPS) and 4,4'-thiodiphenol (THIO), and two new antiglucocorticoids, bisphenol Z and its analog bis[4-(2-hydroxyethoxy)phenyl] sulfone (BHEPS) were identified. Moreover, four new glucocorticoid agonists (methyl paraben, ethyl paraben, propyl paraben and bisphenol F) were found. To elucidate the structure-activity relationship of bisphenols, we performed molecular docking experiments with androgen and glucocorticoid receptor. These docking experiments had shown that bulky structures such as BHEPS and bisphenol Z act as antiglucocorticoid, because they are positioned toward helix H12 in the antagonist conformation and could therefore be responsible for H12 conformational change and the switch between agonistic and antagonistic conformation of receptor. On the other hand smaller structures cannot interact with H12. The results of in vitro screening of fifteen industrial chemicals as modulators of the glucocorticoid and androgen receptor activities demand additional in vivo testing of these chemicals for formulating any relevant hazard identification to human health.

  19. Biocidal and inhibitory activity screening of de novo synthesized surfactants against two eukaryotic and two prokaryotic microbial species.

    Science.gov (United States)

    Tiecco, Matteo; Cardinali, Gianluigi; Roscini, Luca; Germani, Raimondo; Corte, Laura

    2013-11-01

    Thirty-six quaternary ammonium salts, of which 28 structurally different non-commercially available surfactants, were tested to screen their biocidal and inhibitory antimicrobial activity. Their activity was compared to commercially available amphiphiles as well as to non-amphiphilic quaternary ammonium salts. As target of these compounds four microbial species were employed of which two (Saccharomyces cerevisiae and Candida albicans) were important yeast in the food and clinical environment and the other two (Escherichia coli and Listeria innocua) represented the Gram negative and positive bacteria, respectively. The surfactants showed the ability to kill the microbial cells in water solution and to variably hamper their growth onto agar medium. The non-amphiphilic compounds (which represent analogues of some surfactants used in this study, since they have the same head group but no hydrophobic portion) had little effect in solution and no effect against the microbial growth on plate. Amphoteric and non-amphoteric zwitterionic surfactants showed reduced biocidal activity. The most active antimicrobial agent was N-tetradecyltropinium bromide (23S) surfactant. The presence of cells did not significantly affect the ability to form micelles, as demonstrated by comparative conductometric measurements.

  20. 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

  1. Estimating the individual benefit of immediate treatment or active surveillance for prostate cancer after screen-detection in older (65+) men.

    Science.gov (United States)

    de Carvalho, Tiago M; Heijnsdijk, Eveline A M; de Koning, Harry J

    2016-05-15

    A significant proportion of screen-detected men with prostate cancer is likely to be overtreated, especially in older age groups. We aim to find which groups of screen-detected older men (65+) benefit the most from Immediate Radical Treatment or Active Surveillance (AS) for prostate cancer, depending on age, screening history, health status and prostate cancer stage at detection. We used a microsimulation model (MISCAN) of the natural history of prostate cancer based on ERSPC data. Individual life histories are simulated with US comorbidity lifetables based on a random sample of MEDICARE data. Different screening histories are simulated and we count outcomes for men screen-detected from ages 66 to 72. For immediately treated men with low-risk disease (≤ T2a, Gleason 6) the probability of overtreatment ranges from 61% to 86% decreasing to between 37 and 46%, if they are assigned to AS. For intermediate risk men (≤ T2, Gleason 3 + 4) overtreatment ranges from 23 to 60%, which reduces to between 16 and 31% for AS. For high risk men (T3, or ≥ Gleason 4 + 3), overtreatment ranges from 11 to 51%. The disease stage at screen-detection is a critical risk factor for overtreatment. For low risk men, AS seems to significantly reduce overtreatment at a modest cost. For intermediate risk men, the decision between immediate treatment or AS depends on age and comorbidity status. Men screen-detected in a high risk disease stage may benefit from immediate treatment even beyond age 69.

  2. Screening of some medicinal plants from cameroon for beta-lactamase inhibitory activity.

    Science.gov (United States)

    Gangoué-Piéboji, Joseph; Baurin, Stéphane; Frère, Jean-Marie; Ngassam, Pierre; Ngameni, Bathelemy; Azebaze, Anatole; Pegnyemb, Dieudonné Emmanuel; Watchueng, Jean; Goffin, Colette; Galleni, Moreno

    2007-03-01

    In efforts to find new bioactive beta-lactamase inhibitors, this study investigated 16 Cameroonian plants belonging to 10 families which were evaluated for anti-beta-lactamase activity. The investigation showed that extracts 2, 6, 3 and 5 of the 16 plants investigated presented interesting in vitro beta-lactamase inhibition (over 90%), respectively, of the beta-lactamases TEM-1, OXA-10, IMP-1 and P99. These extracts were from Mammea africana (all beta-lactamases), Garcinia lucida, G. kola (OXA-10, IMP-1 and P99), Bridelia micrantha (OXA-10, P99), Ochna afzelii (OXA-10, P99), Prunus africana (IMP-1) and Adenia lobata (TEM-1). After elimination of tannins (according to the European Pharmacopoeia) the extracts from B. micrantha, G. lucida and M. africana were tested further for their anti-beta-lactamase activity. The extracts from B. micrantha and G. lucida exhibited potent inhibitory activity, respectively, of beta-lactamase OXA-10 (IC(50) = 0.02 mg/mL) and P99 (IC(50) = 0.01 mg/mL). The anti-beta-lactamase activity of M. africana extract was weak. The isolation and the structural elucidation of the active constituents of G. lucida and B. micrantha will provide useful leads in the development of beta-lactamase inhibitors.

  3. Phytochemical screening and antiviral activity of some medicinal plants from the island Soqotra.

    Science.gov (United States)

    Mothana, Ramzi A A; Mentel, Renate; Reiss, Christiane; Lindequist, Ulrike

    2006-04-01

    Methanol and hot-aqueous extracts of 25 different plant species, used in Yemeni traditional medicine and growing, partly as endemic plants, on the island Soqotra have been investigated for their antiviral activity. In addition, the phytochemical identification of the main chemical constituents was performed. The extracts were assayed in two in vitro viral systems, which used influenza virus type A/MDCK cells and herpes simplex virus type 1/Vero cells, at non-cytotoxic concentrations. The herpes simplex virus type 1 showed more sensitivity than the influenza virus type A against the extracts investigated. The methanol extracts of Boswellia ameero, Boswellia elongata, Buxus hildebrandtii, Cissus hamaderohensis, Cleome socotrana, Dracaena cinnabari, Exacum affine, Jatropha unicostata and Kalanchoe farinacea showed anti-influenza virus type A activity with 50% inhibition (IC50) concentrations ranging from 0.7 to 12.5 microg/mL. In addition, 17 plants of the 25 investigated exhibited anti-HSV-1 activity. The antiviral activity of some active extracts was also observed on a molecular level.

  4. Sulfonylureas and glinides exhibit peroxisome proliferator-activated receptor gamma activity: A combined virtual screening and biological assay approach

    NARCIS (Netherlands)

    Scarsi, M.; Podvinec, M.; Roth, A.; Hug, H.; Kersten, A.H.; Albrecht, H.; Schwede, T.; Meyer, U.A.; Rucker, C.

    2007-01-01

    Most drugs currently employed in the treatment of type 2 diabetes either target the sulfonylurea receptor stimulating insulin release (sulfonylureas, glinides), or target the peroxisome proliferator-activated receptor (PPAR) improving insulin resistance (thiazolidinediones). Our work shows that sulf

  5. A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activity.

    Directory of Open Access Journals (Sweden)

    Elizabeth R Sharlow

    Full Text Available BACKGROUND: The parasitic protozoan Trypanosoma brucei utilizes glycolysis exclusively for ATP production during infection of the mammalian host. The first step in this metabolic pathway is mediated by hexokinase (TbHK, an enzyme essential to the parasite that transfers the gamma-phospho of ATP to a hexose. Here we describe the identification and confirmation of novel small molecule inhibitors of bacterially expressed TbHK1, one of two TbHKs expressed by T. brucei, using a high throughput screening assay. METHODOLOGY/PRINCIPAL FINDINGS: Exploiting optimized high throughput screening assay procedures, we interrogated 220,233 unique compounds and identified 239 active compounds from which ten small molecules were further characterized. Computation chemical cluster analyses indicated that six compounds were structurally related while the remaining four compounds were classified as unrelated or singletons. All ten compounds were approximately 20-17,000-fold more potent than lonidamine, a previously identified TbHK1 inhibitor. Seven compounds inhibited T. brucei blood stage form parasite growth (0.03activity. None of the compounds displayed structural similarity to known hexokinase inhibitors or human African trypanosomiasis therapeutics. CONCLUSIONS/SIGNIFICANCE: The novel chemotypes identified here could represent leads for future therapeutic development against the African trypanosome.

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

    Directory of Open Access Journals (Sweden)

    David Revalds Lubans

    2014-05-01

    Full Text Available Purpose: The primary aim is to describe the development and implementation of a smartphone application (app designed to promote physical activity and reduce screen-time in adolescent boys ‘at risk’ of obesity from low-income communities.Methods: An app was developed to support the delivery of a face-to-face school-based obesity prevention program known as the ‘Active Teen Leaders Avoiding Screen-time’ (ATLAS program. ATLAS was guided by self-determination theory and social cognitive theory and evaluated using a cluster randomized controlled trial with 361 boys (12.7± 0.5 years in 14 secondary schools. Following the completion of the study, participants in the intervention group completed a process evaluation questionnaire and focus groups were conducted with 42 students to explore their general perceptions of the ATLAS program and their experience with the smartphone app. Barriers and challenges encountered in the development, implementation and evaluation of the app are also described.Results: Participation in the study was not contingent on ownership of a smartphone, but 70% of participants in the intervention group reported having access to a smartphone or tablet device. Focus group participants reported an enjoyment of the program, and felt that it had provided them with new skills, techniques, and routines for the future. However, their engagement with the smartphone app was limited, due to a variety of reasons. Barriers to the implementation and evaluation of the app included limited access to smartphone devices, technical problems with the push notifications, lack of access to usage data and the challenges of maintaining participants’ interest in using the app.Conclusions: Although participants reported high levels of satisfaction with the ATLAS program in general, the smartphone app was not used extensively. Additional strategies and features may be needed to enhance engagement in adolescent boys.

  7. Screening of antibacterial activity of Amaicha del Valle (Tucumán, Argentina) propolis.

    Science.gov (United States)

    Nieva Moreno, M I; Isla, M I; Cudmani, N G; Vattuone, M A; Sampietro, A R

    1999-12-15

    Propolis is extensively used in Argentine folk medicine. Alcoholic extracts of propolis from four localities of Amaicha del Valle (El Paraiso, La Banda Este, La Banda Oeste and El Molino), Province of Tucumán and from Cerrillos, Province of Santiago del Estero, Argentina were prepared. All showed antibacterial activity against Gram positive bacteria, the propolis from La Banda Este being the most active (MIC = 7.8 microg/ml) against Streptococcus piogenes, an antibiotic resistant bacterium. Thin layer chromatographic (TLC) separation profiles of propolis from Amaicha del Valle region were similar but differ from the alcoholic extract of the propolis from Cerrillos, another phytogeographical region of Argentina (provincia chaqueña). Bioautographic assays of the TLC profiles showed that several separated compounds of the Amaicha del Valle propolis have antibacterial activity. The difference in composition between Amaicha del Valle and Cerrillos propolis coincides with a different phytogeographical formation.

  8. Screening of the topical anti-inflammatory activity of some Central American plants.

    Science.gov (United States)

    Sosa, S; Balick, M J; Arvigo, R; Esposito, R G; Pizza, C; Altinier, G; Tubaro, Aurelia

    2002-07-01

    Hexane, chloroform and methanol extracts of seven herbal drugs used in the folk medicine of Central America against skin disorders (Aristolochia trilobata leaves and bark, Bursera simaruba bark, Hamelia patens leaves, Piper amalago leaves, and Syngonium podophyllum leaves and bark) were evaluated for their topical anti-inflammatory activity against the Croton oil-induced ear oedema in mice. Most of the extracts induced a dose-dependent oedema reduction. The chloroform extract of almost all the drugs exhibited interesting activities with ID(50) values ranging between 108 and 498 micro g/cm(2), comparable to that of indomethacin (93 micro g/cm(2)). Therefore, the tested plants are promising sources of principles with high anti-inflammatory activity.

  9. Screening of anti-bacterial activity of medicinal plants from Belize (Central America).

    Science.gov (United States)

    Camporese, A; Balick, M J; Arvigo, R; Esposito, R G; Morsellino, N; De Simone, F; Tubaro, A

    2003-07-01

    Twenty-one extracts from seven herbal drugs, Aristolochia trilobata (Aristolochiaceae) leaves and bark, Bursera simaruba (Burseraceae) bark, Guazuma ulmifolia (Sterculiaceae) bark, Hamelia patens (Rubiaceae) leaves and Syngonium podophyllum (Araceae) leaves and bark, used in traditional medicine of Belize (Central America) as deep and superficial wound healers, were evaluated for their anti-bacterial properties. Activity was tested against standard strains of Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923 and Enterococcus faecalis ATCC 29212. Almost all the extracts were able to inhibit the growth of one or more of the bacterial strains, except that of Enterococcus faecalis. For the first time an anti-microbial activity is reported for Aristolochia trilobata as well as for Syngonium podophyllum. The hexane extracts of Aristolochia trilobata leaves and bark were the most active extracts against Staphylococcus aureus (MIC=0.31 and 0.625mg/ml, respectively).

  10. Phytochemical screening and evaluation of antioxidant activities of Dracocephalum kotschyi and determination of its luteolin content

    Directory of Open Access Journals (Sweden)

    Mansureh Kamali

    2016-06-01

    Full Text Available Objective: Dracocephalum kotschyi (Lamiaceae family has been usedin traditional medicine for stomach and liver disorders, headache and congestion. In the present study, we have investigated phytochemical properties and antioxidant activities of dichloromethane, ethyl acetate and methanol extracts of D.kotschyi. Material and Methods: Antioxidant activities of extracts were evaluated using the integration of HPLC-DPPH and ferric reducing antioxidant power (FRAP methods. In addition, the luteolincontent was determined using HPLC method. Results: The highest antioxidant activity was observed for the methanol extract (among the three tested extracts showing 50% DPPH scavenging activity at 4.85µg/ml as compared to butylated hydroxy toluene (BHT and ascorbic acid (3.00 µg/ml, 0.97 µg/ml. Also, luteolin was detected in methanol extract; it was identified by comparing its retention time and DAD spectra with standard and it was one of antioxidant components of this plant. In addition, the antioxidant activity of methanol extract was higher than BHT, in FRAP assay. Total phenolic content was in the range of 11.62-22.29 mg Gallic acid /gram of dry extract and flavonoid content was in the range of 3.97-5.042 mg             Quercetin/ gram of extract for dichloromethane, ethyl acetate and methanol extracts. The quantity of luteolin in D.kotschyiwas found to be 1061.005 µg/g of dried plant. Conclusion: The results of this investigation indicated that luteolin plays major role in the antioxidant activity of the plant.

  11. Screening test for anti-Helicobacter pylori activity of traditional Chinese herbal medicines

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    AIM:To evaluate the anti-Helicobacter pylori (H.pylori) activity of 50 traditional Chinese herbal medicines in order to provide the primary evidence for their use in clinical practice.METHODS:A susceptibility test of water extract from 50 selected traditional Chinese herbal medicines for in vitro H.pylori Sydney strain 1 was performed with broth dilution method.Anti-H.pylori activity of the selected Chinese herbal medicines was evaluated according to their minimum inhibitory concentration (MIC).RESULTS:The ...

  12. Screening of Fungi from Chinese Medical Plants for Anti-Human Immunodeficiency Virus Type 1 Activity

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    In order to isolate anti-human immunodeficiency virus (HIV) agents from natural products, 97 ethanolic extracts of 90 fungi were tested for their inhibitory activity on HIV-1. Most of the extracts tested were relatively non-toxic to human lymphocytic MT-4 cells, but extracts of some fungi exhibited potent anti-HIV activity in an in vitro 3-(4,5-dimethyl-2 thiazoyl)-2,5-diphenyl-2H-tetrazolium bromide assay with a selectivity index greater than 3. Most fungi were isolated from Dendrobium sp. and Taxus sp.

  13. [SCREENING AND SELECTION OF THE SOIL MICROORGANISMS ON THE ABILITY OF "NITROGEN-FIXING ACTIVITY"].

    Science.gov (United States)

    Patyka V Ph; Kyrychenko, O V; Kots, S Ya

    2015-01-01

    The isolates of microorganisms from the rhizosphere of spring barley plants and soil at the use of analytical selection method was isolated. Its isolates on the ability of "nitrogen-fixing activity" was tested. It was shown that isolates of microorganisms had different of the colonies formed and cultural growth on the Eshbi's selective medium as well as the ability to fixing of molecular nitrogen. The different levels of intensity and dynamics of isolates nitrogenase activity in vitro were identified. New isolates of the soil microorganisms complement of the gene pool diazotrophic bacteria. Its isolates are perspectivity for the study as the basis or components of the bacterial fertilizers for the crops.

  14. Phytochemical screening and antimicrobial activities of the constituents isolated from Koelreuteria paniculata leaves.

    Science.gov (United States)

    Ghahari, Somayeh; Alinezhad, Heshmatollah; Nematzadeh, Ghorban Ali; Ghahari, Sajjad

    2015-01-01

    Methanolic extract of Golden rain leaves was fractionated by column chromatography on silica gel and 18 fractions were obtained. Antimicrobial activities of fractions were investigated against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa as quality control bacteria and fungus Pyricularia grisea which causes Blast disease in rice. Fractions showed more antibacterial activity at 0.04 g/mL concentration only on B. subtilis and S. aureus as gram positive bacteria. Also, three fractions indicated excellent antifungal effect on fungus P. grisea. Moreover, in the present study, fractions that showed very good effect on microorganisms were used for gas chromatography-mass spectrometry analysis to identify different phytochemicals.

  15. [BACILLUS STRAINS'S SCREENING--ACTIVE ANTAGONISTS OF BACTERIAL AND FUNGAL PHYTOPATHOGENS].

    Science.gov (United States)

    Grabova, A Yu; Dragovoz, I V; Kruchkova, L A; Pasichnik, L A; Avdeeva, L V

    2015-01-01

    Antagonistic activity 100 strains of Bacillus bacteria towards to museum and actual strains of phytopathogenic bacteria and fungy was defined. Relation between level of antagonistic activity to phytopathogenic bacteria and genus accessory of the last was shown. The medium level of antagonism to fungal phytopathogens at 30% of the studied strains of Bacillus bacteria was shown. 5 strains of Bacillus sp. with high and medium levels of antagonism to phytopathogens bacterial and fungy nature was selected and considered as perspective for creation of biological preparations for plant protection.

  16. Fe en Accion/Faith in Action: Design and implementation of a church-based randomized trial to promote physical activity and cancer screening among churchgoing Latinas

    Science.gov (United States)

    Arredondo, Elva M.; Haughton, Jessica; Ayala, Guadalupe X.; Slymen, Donald J.; Sallis, James F.; Burke, Kari; Holub, Christina; Chanson, Dayana; Perez, Lilian G.; Valdivia, Rodrigo; Ryan, Sherry; Elder, John

    2015-01-01

    Objectives To describe both conditions of a two-group randomized trial, one that promotes physical activity and one that promotes cancer screening, among churchgoing Latinas. The trial involves promotoras (community health workers) targeting multiple levels of the Ecological Model. This trial builds on formative and pilot research findings. Design Sixteen churches were randomly assigned to either the physical activity intervention or cancer screening comparison condition (approximately 27 women per church). In both conditions, promotoras from each church intervened at the individual- (e.g., beliefs), interpersonal- (e.g., social support), and environmental- (e.g., park features and access to health care) levels to affect change on target behaviors. Measurements The study’s primary outcome is min/wk of moderate-to-vigorous physical activity (MVPA) at baseline and 12 and 24 months following implementation of intervention activities. We enrolled 436 Latinas (aged 18–65 years) who engaged in less than 250 min/wk of MVPA at baseline as assessed by accelerometer, attended church at least four times per month, lived near their church, and did not have a health condition that could prevent them from participating in physical activity. Participants were asked to complete measures assessing physical activity and cancer screening as well as their correlates at 12- and 24-months. Summary Findings from the current study will address gaps in research by showing the long term effectiveness of multi-level faith-based interventions promoting physical activity and cancer screening among Latino communities. PMID:26358535

  17. Screening a Mediterranean Sponge Axinella verrucosa For Antibacterial Activity in Comparison to Some Antibiotics

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    Alma Shabbar

    2013-03-01

    Full Text Available The antibacterial effect of crude extract of marine sponge Axinella verrucosa at room temperature against seven nosocomial bacteria and one fungal isolates including, Staphylococcus aureus, Pseudomonas aeruginosa, Acinetobacter septicus and Proteus vulgaris, Acinetobacter meningitis, Klebsiella pneumonia, E. coli and the fungal pathogen Candida albicans were studied by Kirby-Bauer disc diffusion assay and, the findings of antibacterial activity of crude methanolic extract sponge A. verrucosa were compared to the efficiency of some marketed antibiotics that were tested against the same bacteria at given concentrations. In result, it was found that MeOH crude extract of Axinella verrucosa is effective against Staphylococcus aureus, Pseudomonas aeruginosa, Acinetobacter septicus and Proteus vulgaris and except for its ineffectiveness against Acinetobacter meningitis, Klebsiella pneumonia, E. coli and the fungal pathogen Candida albicans. It was more active than Azithromycin and Gentamicin Against Proteus vulgaris and more efficient than ciprofloxacin against Acinetobacter septicus. Hexane and Ethyl acetate crude extracts derived from A. verrucosa revealed no activity against all bacterial and fungal pathogen. Sponge Axinella verrucosa remains an interesting source of new antibacterial metabolites with better activity than some antibiotics.

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

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    Naveed Muhammad

    2013-03-01

    Conclusions: In vivo studies of SLO showed prominent antinociceptive and antipyretic activities with ample safety profile and thus provided pharmacological base for the traditional uses of the plant in various painful conditions and pyrexia. Additional detail studies are required to ascertain its clinical application.

  19. Screening Neuropharmacological Activities of Kaempferia parviflora (Krachai Dam in Healthy Adult Male Rats

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    Thaneeya Hawiset

    2011-01-01

    Full Text Available Problem statement: Although the global prevalence of psychological disorders is increasing continually, the efficacies of therapeutic strategies are still very limited. Oxidative stress has been implicated in the pathogenesis of psychiatric disorders and substance possessing antioxidant activity can alleviate the mentioned conditions. Therefore, we hypothesized that Kaempferia parviflora, a medicinal plant claimed for nerve tonic, also possessed the neuropharmacological activities which provide the advantage for psychiatric disorders. Approach: Adult male Wistar rats, weighing 180-220 grams, were orally given the ethanolic extract of K. parviflora at doses of 150, 200 and 250 mg kg-1 BW once daily for 2 weeks. Then, they were determined the neuropharmacological activities including anxiolytic, anti-depression like behavior and cognitive enhancement after single dose, 1 and 2 weeks of treatment. Results: K. parviflora possessed anti-depression like behavior and cognitive enhancement at all treatment duration. Unfortunately, this substance failed to show anxiolytic like activity. Conclusion: Our results suggested that K. parviflora might be used as a novel therapeutic strategy for psychiatric disorder and cognitive enhancement. However, further investigations about precise underlying mechanism are still required.

  20. Screening of BADH Activity of Borreria articularies (Linn. for the Inhibition of P. aeruginosa

    Di