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Sample records for activity screen time

  1. Associations between Screen Time and Physical Activity among Spanish Adolescents

    PubMed Central

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

    2011-01-01

    Background Excessive time in front of a single or several screens could explain a displacement of physical activity. The present study aimed at determining whether screen-time is associated with a reduced level of moderate to vigorous physical activity (MVPA) in Spanish adolescents living in favorable environmental conditions. Methodology/Principal Findings A multi-stage stratified random sampling method was used to select 3503 adolescents (12–18 years old) from the school population of Gran Canaria, Spain. MVPA, screen-time in front of television, computer, video game console and portable console was assessed in the classroom by fulfilling a standardized questionnaire. Bivariate and multivariate logistic regression analyses adjusted by a set of social-environmental variables were carried out. Forty-six percent of girls (95% CI±2.3%) and 26% of boys (95% CI±2.1%) did not meet the MVPA recommendations for adolescents. Major gender differences were observed in the time devoted to vigorous PA, video games and the total time spent on screen-based activities. Boys who reported 4 hours•week−1 or more to total screen-time showed a 64% (OR = 0.61, 95% CI, 0.44–0.86) increased risk of failing to achieve the recommended adolescent MVPA level. Participation in organized physical activities and sports competitions were more strongly associated with MVPA than screen-related behaviors. Conclusions/Significance No single screen-related behavior explained the reduction of MVPA in adolescents. However, the total time accumulated through several screen-related behaviors was negatively associated with MVPA level in boys. This association could be due to lower availability of time for exercise as the time devoted to sedentary screen-time activities increases. Participation in organized physical activities seems to counteract the negative impact of excessive time in front of screens on physical activity. PMID:21909435

  2. Screen time and children

    MedlinePlus

    "Screen time" is a term used for activities done in front of a screen, such as watching TV, working on a computer, or playing video games. Screen time is sedentary activity, meaning you are being physically ...

  3. Active versus Passive Screen Time for Young Children

    ERIC Educational Resources Information Center

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

    2012-01-01

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

  4. Screen time and children

    MedlinePlus

    ... screen, such as watching TV, working on a computer, or playing video games. Screen time is sedentary activity, meaning you are ... child eat while watching TV or using the computer. DO NOT leave the ... as family board games, puzzles, or going for a walk. Keep a ...

  5. Leisure time physical activity, screen time, social background, and environmental variables in adolescents.

    PubMed

    Mota, Jorge; Gomes, Helena; Almeida, Mariana; Ribeiro, José Carlos; Santos, Maria Paula

    2007-08-01

    This study analyzes the relationships between leisure time physical activity (LTPA), sedentary behaviors, socioeconomic status, and perceived environmental variables. The sample comprised 815 girls and 746 boys. In girls, non-LTPA participants reported significantly more screen time. Girls with safety concerns were more likely to be in the non-LTPA group (OR = 0.60) and those who agreed with the importance of aesthetics were more likely to be in the active-LTPA group (OR = 1.59). In girls, an increase of 1 hr of TV watching was a significant predictor of non-LTPA (OR = 0.38). LTPA for girls, but not for boys, seems to be influenced by certain modifiable factors of the built environment, as well as by time watching TV. PMID:18019587

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

    PubMed Central

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

    2014-01-01

    Objective: To examine relationships between parenting styles and practices and child moderate-to-vigorous physical activity (MVPA) and screen time. Methods: Participants were children (6.9 ± 1.8 years) with a body mass index in the 70–95th percentile and their parents (421 dyads). Parent-completed questionnaires assessed parental support for child physical activity (PA), parenting styles and child screen time. Children wore accelerometers to assess MVPA. Results: Parenting style did not predict MVPA, but support for PA did (positive association). The association between support and MVPA, moreover, varied as a function of permissive parenting. For parents high in permissiveness, the association was positive (greater support was related to greater MVPA and therefore protective). For parents low in permissiveness, the association was neutral; support did not matter. Authoritarian and permissive parenting styles were both associated with greater screen time. Conclusions: Parenting practices and styles should be considered jointly, offering implications for tailored interventions. PMID:24812256

  7. Changes in screen time activity in Norwegian children from 2001 to 2008: two cross sectional studies

    PubMed Central

    2013-01-01

    Background There has been an increase in screen-based communication, leading to concerns about the negative health effects of screen-based activities in children and adolescents. The present study aimed to (1) analyze changes in screen time activity in Norwegian children from 2001 to 2008, and (2) to analyze associations between the changes in screen time activity over time and sex, grade level and parental educational level. Methods Within the project Fruits and Vegetables Make the Marks (FVMM), 1488 6th and 7th grade pupils from 27 Norwegian elementary schools completed a questionnaire including a question about time spent on television viewing and personal computer use in 2001 and 1339 pupils from the same schools completed the same questionnaire in 2008. Data were analyzed by multilevel linear mixed models. Results The proportions of 6th and 7th grade pupils at the 27 schools that reported screen time activity outside school of 2 hours/day or more decreased from 55% to 45% (p<0.001) from 2001 to 2008 when adjusting for sex, grade level and parental education. The decrease was most evident in 6th graders (51% to 37%) and in children with highly educated parents (54% to 39%). Conclusion The present study shows that there has been a marked reduction in screen time activity outside school in this group of Norwegian 10–12 year olds from 2001 to 2008. PMID:23356930

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

    PubMed Central

    2010-01-01

    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 0.43-0.87; young children OR 0

  9. Concurrent Associations between Physical Activity, Screen Time, and Sleep Duration with Childhood Obesity

    PubMed Central

    Laurson, Kelly R.; Lee, Joey A.; Gentile, Douglas A.; Walsh, David A.; Eisenmann, Joey C.

    2014-01-01

    Aim. To examine the simultaneous influence of physical activity, screen time, and sleep duration recommendations on the odds of childhood obesity (including overweight). Methods. Physical activity was assessed via pedometer and screen time, and sleep duration were assessed via survey in a cross sectional sample of 674 children (aged 7–12 years) from two Midwestern communities in the fall of 2005. Participants were cross tabulated into four groups depending on how many recommendations were being met (0, 1, 2, or all 3). Linear and logistic regression were used to examine the influence of physical activity, screen time and sleep duration on obesity and interactions among the three variables. Results. Children achieving all three recommendations simultaneously (9.2% of total sample) were the least likely to be obese. Approximately 16% of boys and 9% of girls achieving all recommendations were overweight or obese compared to 53% of boys and 42.5% of girls not achieving any. Conclusions. The odds of obesity increased in a graded manner for each recommendation which was not met. Meeting all three recommendations appears to have a protective effect against obesity. Continued efforts are warranted to promote healthy lifestyle behaviors that include meeting physical activity, screen time, and sleep duration recommendations concurrently. PMID:24734210

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

    PubMed Central

    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. PMID:25874123

  11. Home environment relationships with children’s physical activity, sedentary time, and screen time by socioeconomic status

    PubMed Central

    2012-01-01

    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. PMID:22835155

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

    PubMed

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

    2014-12-01

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

  13. The Relationship Between Parental Physical Activity and Screen Time Behaviors and the Behaviors of their Young Children.

    PubMed

    Carson, Valerie; Stearns, Jodie; Janssen, Ian

    2015-08-01

    The main purpose of this study was to examine the relationships between parental and children's physical activity and screen time behaviors in a large sample of children in the early years. The results are based on 738 children aged 0-5 years and their parents from the Kingston, Canada area. Parents completed a questionnaire from May to September 2011 that assessed sociodemographic characteristics, their physical activity and screen time, and their child's physical activity and screen time. Logistic regression models, adjusted for potential confounders, were conducted. Parents in the lowest quartile of physical activity were 2.77 (95% confidence interval (CI): 1.68-4.57) times more likely to have a child in the lowest quartile of physical activity compared with parents in the highest quartile of physical activity. Relationships were stronger in two parent homes compared with single-parent homes. Parents in the second (odds ratio = 2.27, 95% CI: 1.36-3.78), third (2.30, 1.32-3.99), and fourth (7.47, 4.53-12.33) screen time quartiles were significantly more likely to have a child in the highest quartile of screen time compared with parents in quartile one. To optimize healthy growth and development in the early years, future family-centered interventions targeting both physical activity and screen time appear important. PMID:25918825

  14. Promoting active lifestyles in young children: investigating mothers' decisions about their child's physical activity and screen time behaviours.

    PubMed

    Hamilton, Kyra; Thomson, Courtney E; White, Katherine M

    2013-07-01

    Given increasing trends of obesity being noted from early in life and that active lifestyles track across time, it is important that children at a very young age be active to combat a foundation of unhealthy behaviours forming. This study investigated, within a theory of planned behaviour (TPB) framework, factors which influence mothers' decisions about their child's (1) adequate physical activity (PA) and (2) limited screen time behaviours. Mothers (N = 162) completed a main questionnaire, via on-line or paper-based administration, which comprised standard TPB items in addition to measures of planning and background demographic variables. One week later, consenting mothers completed a follow-up telephone questionnaire which assessed the decisions they had made regarding their child's PA and screen time behaviours during the previous week. Hierarchical multiple regression analyses revealed support for the predictive model, explaining an overall 73 and 78 % of the variance in mothers' intention and 38 and 53 % of the variance in mothers' decisions to ensure their child engages in adequate PA and limited screen time, respectively. Attitude and subjective norms predicted intention in both target behaviours, as did intentions with behaviour. Contrary to predictions, perceived behavioural control (PBC) in PA behaviour and planning in screen time behaviour were not significant predictors of intention, neither was PBC a predictor of either behaviour. The findings illustrate the various roles that psycho-social factors play in mothers' decisions to ensure their child engages in active lifestyle behaviours which can help to inform future intervention programs aimed at combating very young children's inactivity. PMID:22833334

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

    PubMed

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

    2015-08-01

    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. PMID:26264005

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

    PubMed Central

    Wijtzes, Anne; van de Bongardt, Daphne; van de Looij-Jansen, Petra; Bannink, Rienke; Raat, Hein

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

  17. Development of HomeSTEAD’s physical activity and screen time physical environment inventory

    PubMed Central

    2013-01-01

    Background The home environment has a significant influence on children’s physical activity, sedentary behavior, dietary intake, and risk for obesity and chronic disease. Our understanding of the most influential factors and how they interact and impact child behavior is limited by current measurement tools, specifically the lack of a comprehensive instrument. HomeSTEAD (the Home Self-administered Tool for Environmental assessment of Activity and Diet) was designed to address this gap. This new tool contains four sections: home physical activity and media equipment inventory, family physical activity and screen time practices, home food inventory, and family food practices. This paper will describe HomeSTEAD’s development and present reliability and validity evidence for the first section. Methods The ANGELO framework guided instrument development, and systematic literature reviews helped identify existing items or scales for possible inclusion. Refinement of items was based on expert review and cognitive interviews. Parents of children ages 3–12 years (n = 125) completed the HomeSTEAD survey on three separate occasions over 12–18 days (Time 1, 2, and 3). The Time 1 survey also collected demographic information and parent report of child behaviors. Between Time 1 and 2, staff conducted an in-home observation and measured parent and child BMI. Kappa and intra-class correlations were used to examine reliability (test-retest) and validity (criterion and construct). Results Reliability and validity was strong for most items (97% having ICC > 0.60 and 72% having r > 0.50, respectively). Items with lower reliability generally had low variation between people. Lower validity estimates (r < 0.30) were more common for items that assessed usability and accessibility, with observers generally rating usability and accessibility lower than parents. Small to moderate, but meaningful, correlations between physical environment factors and BMI, outside

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

    PubMed

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

    2016-04-01

    Objective The purpose of this study was to examine how lifestyle behaviors in the context of physical activity levels and screen time are associated with school absenteeism. Methods We analyzed 2005-2008 NHANES data of proxy interviews for 1048 children aged 6-11 years and in-person self-reports of 1117 adolescents aged 12-18 years. Missing 10% of school days during the past school year was defined as severe school absenteeism (SSA). Results Watching TV ≥2 hours a day was significantly associated with SSA among both children (OR = 3.51 [1.03-12.0]) and adolescents (OR = 3.96 [1.84-8.52]) compared with their peers watching <2 hours a day. A U-shaped association was identified between the level of physical activity and SSA among children. Both inactive children (OR = 12.4 [1.43-108]) and highly active children (14.8 [2.82-77.7]) had higher odds of SSA compared with children with medium levels of physical activity. No associations were observed for either children 0.57 ([0.16-1.99]) or adolescents (0.94 [0.44-2.03]) using a computer ≥3 hours a day. Limitations Cross-sectional study involving self-reports. Transportation to and from school not included in physical activity assessment. Absenteeism was not validated with report cards. Unable to account for the absence type or frequency of illness or injury. No psychometric properties provided for subjective measures regarding participants' attitudes and characteristic traits towards physical activity, TV viewing, and school attendance. Conclusions Excessive TV watching among children and adolescents, and inactivity and high activity levels (≥7 times per week) among children are independently associated with severe school absenteeism. PMID:26700770

  19. Barriers to physical activity in children with autism spectrum disorders: Relationship to physical activity and screen time

    PubMed Central

    Must, A.; Phillips, S. M.; Carol, Curtin; Bandini, L. G.

    2014-01-01

    Background Individual, social, and community barriers to physical activity (PA) experienced by children with autism spectrum disorder (ASD) make PA participation more difficult and may contribute to increased screen time. Methods We compared the prevalence of parent-reported barriers to PA among 58 typically developing (TD) children and 53 children with an ASD, 3-11 years, and assessed the association between barriers and PA participation and screen time among children with ASD. Results Parents of children with ASD reported significantly more barriers than parents of TD children. Based on parent-report, 60% of children with ASD required too much supervision compared to no TD children (p<0.001). Parents of children with ASD were more likely to report that adults lack skills needed to include their child (58%), that their child has few friends (45%), and that other children exclude their child (23%). The number of parent-reported barriers to PA was inversely correlated with the hours spent in PA per year (r=−0.27, p=0.05) and positively related to total screen time (r=0.32, p<0.03). Conclusions These findings underscore the need for community-based PA programs designed to meet the special requirements of this population and policies that compel schools and other government-supported organizations for inclusion and/or targeted programming. PMID:25920014

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

    PubMed Central

    2012-01-01

    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 <12 months) and eight groups of parents with preschool-aged (3–5 year old) children (n=36) in Melbourne, Australia. 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. PMID:23270548

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

    PubMed Central

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

    2014-01-01

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

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

    PubMed

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

    2015-01-01

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

  3. [Physical activity, screen time, and use of medicines among adolescents: the 1993 Pelotas (Brazil) birth cohort study].

    PubMed

    Bergmann, Gabriel Gustavo; Bertoldi, Andréa Dâmaso; Mielke, Grégore Iven; Camargo, Aline Lins; Matijasevich, Alicia; Hallal, Pedro Curi

    2016-01-01

    This study aimed to evaluate cross-sectional and longitudinal associations between physical activity, screen time, and use of medicines among adolescents from the 1993 Pelotas (Brazil) birth cohort study, followed at 11 (N = 4,452), 15 (N = 4,325), and 18 years of age (N = 4,106). The study recorded the use of medicines in the previous 15 days, continuous use of some medication, level of physical activity (by questionnaire and accelerometry), and screen time (TV, computer, and videogame). One-third of adolescents had used at least one medicine in the previous 15 days and approximately 10% were on some continuous medication. In the adjusted analysis, the results showed that higher levels of physical activity at 18 years and less screen time at 15 years in boys were associated with lower overall use of medicines (p < 0.05). For boys, physical activity at 11 and 18 years were inversely related to continuous medication (p < 0.05). More physically active boys and those with less screen time in adolescence showed lower use of medicines at 18 years of age. PMID:27167041

  4. Examining the bidirectional relationship between physical activity, screen time, and symptoms of anxiety and depression over time during adolescence.

    PubMed

    Gunnell, Katie E; Flament, Martine F; Buchholz, Annick; Henderson, Katherine A; Obeid, Nicole; Schubert, Nicholas; Goldfield, Gary S

    2016-07-01

    More physical activity (PA) and less screen time (ST) are positively associated with mental health in adolescents; however, research is limited by short-term designs and the exclusion of ST when examining PA. We examined: (a) changes in PA, ST, symptoms of depression, and symptoms of anxiety over four assessments spanning 11years, and (b) bidirectional relationships between initial PA, ST, and symptoms of depression and anxiety as predictors of change in each other during adolescence. Between 2006 and 2010, participants from Ottawa Canada (Time1; N=1160, Mean age=13.54years) completed questionnaires at four points covering the ages from 10 to 21years. Latent growth modeling was used. PA decreased over time whereas ST and symptoms of depression and anxiety increased over time. Controlling for sex, ethnicity, school location, zBMI, birth year, and parents' education, initially higher anxiety was associated with initially higher ST (covariance=.88, p<.05) and initially lower PA (covariance=-6.84, p=.07) independent of initial symptoms of depression. Higher initial depression was associated with higher initial ST (covariance=2.55, p<.05). Increases in anxiety were associated with increases in ST (covariance=.07, p=.06) and increases in depression (covariance=.41, p<.05). Examining bidirectional relationships, higher initial symptoms of depression predicted greater decreases in PA (b=-.28, p<.05). No other significant findings between initial PA, ST, anxiety, or depression were found as predictors of change in each other. Interventions targeting depression around age 13 may be useful to prevent further declines in PA. Similarly, interventions to reduce ST may be beneficial for concurrent reductions in symptoms of depression and anxiety, irrespective of PA. PMID:27090920

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

    PubMed

    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 < .01) and mothers' control (p < .001) were significantly associated with child weight status. Fathers' reinforcement (p < .01) was significantly associated with child physical activity. For screen-time, mothers' monitoring (p < .001) and child characteristics [age (p = .01), sex (p = .01), BMI z-score (p = .03)] were significant predictors. Mothers' 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. PMID:24751915

  6. Associations of Physical Activity, Screen Time with Depression, Anxiety and Sleep Quality among Chinese College Freshmen

    PubMed Central

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

    2014-01-01

    Objectives 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. Methods 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. Results 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. Conclusions 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. PMID:24964250

  7. A cross-sectional study of the environment, physical activity, and screen time among young children and their parents

    PubMed Central

    2014-01-01

    Background To develop evidence-based interventions promoting healthy active lifestyles among young children and their parents, a greater understanding is needed of the correlates of physical activity and screen time in these dyads. Physical environment features within neighborhoods may have important influences on both children and their parents. The purpose of this study was to examine the associations between several features of the physical environment with physical activity and screen time among 511 young children (≤5 years old) and their parents, after adjusting for socio-demographic factors. Methods From May to September, 2011, parents of 0–5 year old children from Kingston, Canada completed a questionnaire that assessed socio-demographic characteristics, their physical activity and screen time, and their child’s physical activity and screen time. Guided by a previously developed conceptual framework, several physical environment features were assessed using Geographic Information Systems including, function (walkability), safety (road speed), aesthetics (streetscape), and destination (outdoor play/activity space, recreation facilities, distance to closest park, yard at home). Multilevel linear regression analyses were used to examine the relationships while adjusting for several socio-demographic factors. Results The only independent association observed for the physical environment features was between higher outdoor play/activity space and higher screen time levels among parents. Several associations were observed with socio-demographic variables. For physical activity, child age, child care status, and family socioeconomic status (SES) were independent correlates for children while sex was an independent correlate for parents. For screen time, child age and family SES were independent correlates for children while neighborhood SES was an independent correlate for parents. Conclusions The findings suggest that socio-demographic factors, including

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

    PubMed

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

    2014-03-01

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

  9. Influence of a health education intervention on physical activity and screen time in primary school children: 'Switch Off--Get Active'.

    PubMed

    Harrison, Michael; Burns, Con F; McGuinness, Meabh; Heslin, Julie; Murphy, Niamh M

    2006-10-01

    Low levels of physical activity coupled with high levels of television viewing have been linked with obesity in children. The objective of this study was to assess the efficacy of 'Switch Off-Get Active', a 16-week controlled health education intervention, in increasing physical activity and reducing screen time and BMI in primary school children. A secondary objective was to compare children with high and low screen time. Participants were 312 children aged 10.2+/-0.7 years, attending nine schools in areas of social disadvantage. The 10-lesson, teacher-led intervention, conducted in spring 2003, emphasised self-monitoring, budgeting of time and selective viewing. Differences, adjusted for baseline values by ANCOVA, existed between intervention and control children at follow-up for self-reported physical activity (intervention +0.84 30 min blocks/day, 95%CI 0.11-1.57, p<0.05) and self-efficacy for physical activity (p<0.05) but not self-reported screen time (intervention--0.41 blocks/day, 95%CI--0.93-0.12, p=0.13) or BMI (p=0.63). Cross-sectional comparisons at baseline indicated lower physical activity, self-efficacy for physical activity and aerobic fitness and a higher BMI in children with high screen time. In conclusion, health education interventions can increase physical activity in primary school children but follow-ups of longer duration may be needed to demonstrate intervention effects on BMI. PMID:16872900

  10. The Activated Coagulation Time of Whole Blood as a Routine Pre-Operative Screening Test

    PubMed Central

    Hattersley, Paul G.

    1971-01-01

    Patients with disorders of hemostasis who undergo surgical procedures are in danger of hemorrhage. While the careful medical history remains the most sensitive test of a bleeding tendency, some such patients can give no suggestive history. In three patients with coagulopathy—one with mild classical hemophilia, one with Christmas disease, and one with warfarin toxicity—the abnormality was missed by routine preoperative history but promptly detected by the routine preoperative use of the activated coagulation time (act). Either this test or the activated partial thromboplastin time should be included in the routine preoperative work-up, along with appropriate additional tests of the hemostatic mechanism. PMID:5087876

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

    PubMed

    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 < .0001) and females (p < .0001). Greater levels of friends' screen time was associated with greater levels of screen time in males (p = .04) while psychosocial variables, such as increased screen time enjoyment, were associated with increased screen time in females (p = .01). School level was not associated with either MVPA or screen time. Focus group data indicated that friends positively influenced participants' MVPA through engaging in activity with participants, verbal encouragement, and modeling of MVPA. All participants preferred to be active with friends rather than alone, however, females preferred activity with a close friend while males preferred to be active with a group. Enjoyment of MVPA was the most cited reason for engaging in MVPA with friends. The majority of participants reported friends not having an influence on screen time. Adolescents with active friends are more likely to be physically active and spend less time engaging in

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

    PubMed Central

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

    2015-01-01

    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. PMID:26264005

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

    PubMed Central

    Silver, Lynn D.; Kettel Khan, Laura; Leviton, Laura

    2014-01-01

    Childhood obesity is associated with health risks in childhood, and it increases the risk of adult obesity, which is associated with many chronic diseases. Therefore, implementing policies that may prevent obesity at young ages is important. In 2007, the New York City Department of Health and Mental Hygiene implemented new regulations for early childhood centers to increase physical activity, limit screen time, and provide healthful beverage offerings (ie, restrict sugar-sweetened beverages for all children, restrict whole milk for those older than 2 years, restrict juice to beverages that are 100% juice and limit serving of juice to only 6 ounces per day, and make water available and accessible at all times). This article explains why these amendments to the Health Code were created, how information about these changes was disseminated, and what training programs were used to help ensure implementation, particularly in high-need neighborhoods. PMID:25321633

  14. Parenting Style, the Home Environment, and Screen Time of 5-Year-Old Children; The ‘Be Active, Eat Right’ Study

    PubMed Central

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

    2014-01-01

    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. PMID:24533092

  15. Evaluation design of New York City's regulations on nutrition, physical activity, and screen time in early child care centers.

    PubMed

    Breck, Andrew; Goodman, Ken; Dunn, Lillian; Stephens, Robert L; Dawkins, Nicola; Dixon, Beth; Jernigan, Jan; Kakietek, Jakub; Lesesne, Catherine; Lessard, Laura; Nonas, Cathy; O'Dell, Sarah Abood; Osuji, Thearis A; Bronson, Bernice; Xu, Ye; Kettel Khan, Laura

    2014-01-01

    This article describes the multi-method cross-sectional design used to evaluate New York City Department of Health and Mental Hygiene's regulations of nutrition, physical activity, and screen time for children aged 3 years or older in licensed group child care centers. The Center Evaluation Component collected data from a stratified random sample of 176 licensed group child care centers in New York City. Compliance with the regulations was measured through a review of center records, a facility inventory, and interviews of center directors, lead teachers, and food service staff. The Classroom Evaluation Component included an observational and biometric study of a sample of approximately 1,400 children aged 3 or 4 years attending 110 child care centers and was designed to complement the center component at the classroom and child level. The study methodology detailed in this paper may aid researchers in designing policy evaluation studies that can inform other jurisdictions considering similar policies. PMID:25321635

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

    PubMed Central

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

    2014-01-01

    Purpose: To describe the development and implementation of a smartphone application (app) designed to promote physical activity and reduce screen-time in adolescent boys considered “at-risk” of obesity. Methods: An app was developed to support the delivery of a face-to-face school-based obesity prevention program known as the “Active Teen Leaders Avoiding Screen-time” (ATLAS) program. ATLAS was guided by self-determination theory and social cognitive theory and evaluated using a cluster 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. Conclusion: 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. PMID:24904909

  17. Do specific parenting practices and related parental self-efficacy associate with physical activity and screen time among primary schoolchildren? A cross-sectional study in Belgium

    PubMed Central

    De Lepeleere, Sara; De Bourdeaudhuij, Ilse; Cardon, Greet; Verloigne, Maïté

    2015-01-01

    Objectives To assess the association between specific parenting practices and related parental self-efficacy with children's physical activity (PA) and screen time. Parental body mass index (BMI), family socioeconomic status (SES), and child's age and gender were examined as possible influencing factors. Design Cross-sectional. Setting January 2014, Flanders (Belgium). Participants 207 parents (87.4% mothers) of children aged 6–12 years. Outcome measures Specific parenting practices, related parental self-efficacy, and children's PA and screen time. Results The majority of investigated parenting practices and related parental self-efficacy were not significantly associated with children's PA or screen time. However, children were more physically active if sports equipment was available at home (p<0.10) and if parents did not find it difficult to motivate their child to be physically active (p<0.05). Children had a lower screen time if parents limited their own gaming (p<0.01). The associations between parenting practices and related parental self-efficacy with children's PA or screen time were significant for parents with a normal BMI, for medium-high SES families and for parents of younger children. Furthermore, the association between the parenting relating factors and children's PA and screen time differed for boys and girls. Conclusions In contrast to what we expected, the findings of the current study show that only a very few specific parenting practices and related parental self-efficacy were associated with children's PA and screen time. It was expected that parental self-efficacy would play a more important role. This can be due to the fact that parental self-efficacy was already high in this group of parents. Therefore, it is possible that parents do not realise how difficult it is to perform certain parenting practices until they are faced with it in an intervention. Trial registration number EC/2012/317. PMID:26346871

  18. Adiposity and Different Types of Screen Time

    PubMed Central

    Rosner, Bernard; Willett, Walter C.; Sonneville, Kendrin R.; Hu, Frank B.; Field, Alison E.

    2013-01-01

    OBJECTIVE: Few prospective studies have examined separate forms of screen time in relation to adiposity. Our objective was to assess independent relations of television, electronic games (video/computer), and digital versatile disc (DVD)/videos and total screen time with change in adolescent BMI. METHODS: Using data from the 2004, 2006, and 2008 waves of the ongoing Growing up Today Study II, we assessed baseline and 2-year change in reported screen time in relation to concurrent change in BMI among 4287 girls and 3505 boys aged 9 to 16 years in 2004. Gender-specific models adjusted for previous BMI, age, race/ethnicity, growth/development, months between questionnaires, and physical activity. RESULTS: Among girls and boys, each hour per day increase in reported television viewing was associated with a 0.09 increase in BMI (Ps < .001), and each hour per day increase in total screen time was associated with a 0.07 increase among girls and 0.05 increase among boys (Ps < .001). Among girls only, greater baseline television, games, and total screen time and change in DVDs/videos were associated with gains in BMI (Ps < .05). BMI gains associated with change in television and total screen time were stronger among overweight girls than lean girls (Ps-heterogeneity < .001). CONCLUSIONS: Television, which remains the steadiest source of food advertising, was most consistently associated with BMI gains. Among girls, electronic games and DVDs/videos were also related to increased BMI, possibly due to influences of product placements and advergames on diet and/or distracted eating. Adolescents, especially overweight adolescents, may benefit from reduced time with multiple types of media. PMID:24276840

  19. Joint association of physical activity/screen time and diet on CVD risk factors in 10-year-old children.

    PubMed

    Drenowatz, Clemens; Carlson, Joseph J; Pfeiffer, Karin A; Eisenmann, Joey C

    2012-12-01

    The increasing prevalence of childhood overweight and obesity has been associated with an increased risk for cardiovascular disease (CVD). While several studies examined the effect of single behaviors such as physical activity (PA), sedentary behavior or diet on CVD risk, there is a lack of research on combined associations, specifically in children. Therefore, the purpose of this study was to examine the joint association of PA or screen time (ST) and diet on CVD risk factors in children. PA, STand diet were assessed via questionnaire in 210 fifth grade students (age: 10.6 ± 0.4 years). The healthy eating index (HEI) was subsequently calculated as indicator for diet quality. Height, weight, % body fat, and resting blood pressure were measured according to standard procedures and blood samples obtained via fingerprick were assayed for blood lipids. Total cholesterol HDL ratio (TC:HDL), mean arterial pressure (MAP), and % body fat were used as indicators of CVD risk. 55% of children did not meet current PA recommendations on at least 5 days/week and 70% exceeded current recommendations for ST. Further, only 2.5% possessed a "good" diet (HEI> 80). There was no significant association of PA or STand diet on CVD risk score. Neither TC:HDL, MAP, and % body fat nor the total CVD risk score was significantly correlated with diet, PA, or ST. Children in the high PA group, however, had significantly better diet scores. Despite the fact that self-reported PA, ST, or dietary intake were not directly related to CVD risk in this sample, higher activity levels were associated with a healthier diet and lower ST indicating an overall healthier lifestyle of this subgroup. PMID:23224418

  20. The Effects of Leisure-Based Screen Time

    ERIC Educational Resources Information Center

    Meier, Mary Dawn; Hager, Ronald L.; Vincent, Susan D.; Tucker, Larry A.; Vincent, William J.

    2007-01-01

    Background: Use of television, computers, and video games competes with physical activity and may be a health risk factor. Purpose: This study assessed the relationship between leisure-based screen time and physical activity in families to determine whether assignment to a limited screen time group results in more physical activity. Methods:…

  1. Relationship between leisure time screen activity and aggressive and violent behaviour in Iranian children and adolescents: the CASPIAN-IV Study.

    PubMed

    Kelishadi, Roya; Qorbani, Mostafa; Motlagh, Mohammad Esmaeil; Heshmat, Ramin; Ardalan, Gelayol; Jari, Mohsen

    2014-08-21

    Background: This study aimed to assess the relationship between leisure time spent watching television (TV) and at a computer and aggressive and violent behaviour in children and adolescents. Methods: In this nationwide study, 14,880 school students, aged 6-18 years, were selected by cluster and stratified multi-stage sampling method from 30 provinces in Iran. The World Health Organization Global School-based Health Survey questionnaire (WHO-GSHS) was used. Results: Overall, 13,486 children and adolescents (50·8% boys, 75·6% urban residents) completed the study (participation rate 90·6%). The risk of physical fighting and quarrels increased by 29% (OR 1·29, 95% CI 1·19-1·40) with watching TV for >2 hr/day, by 38% (OR 1·38, 95% CI 1·21-1·57) with leisure time computer work of >2 hr/day, and by 42% (OR 1·42, 95% CI 1·28-1·58) with the total screen time of >2 hr/day. Watching TV or leisure time spent on a computer or total screen time of >2 hr/day increased the risk of bullying by 30% (OR 1·30, 95% CI 1·18-1·43), 57% (1·57, 95% CI 1·34-1·85) and 62% (OR 1·62, 95% CI 1·43-1·83). Spending >2 hr/day watching TV and total screen time increased the risk of being bullied by 12% (OR 1·12, 95% CI 1·02-1·22) and 15% (OR 1·15, 95% CI 1·02-1·28), respectively. This relationship was not statistically significant for leisure time spent on a computer (OR 1·10, 95% CI 0·9-1·27). Conclusions: Prolonged leisure time spent on screen activities is associated with violent and aggressive behaviour in children and adolescents. In addition to the duration of screen time, the association is likely to be explained also by the media content. PMID:25146837

  2. A Bioactivity-Based Method for Screening, Identification of Lipase Inhibitors, and Clarifying the Effects of Processing Time on Lipase Inhibitory Activity of Polygonum Multiflorum.

    PubMed

    Chang, Yan-Xu; Ge, Ai-Hua; Jiang, Yan; Teye Azietaku, John; Li, Jin; Gao, Xiu-Mei

    2016-01-01

    Traditional Chinese medicine (TCM) has been used for the treatment of many complex diseases. However, the bioactive components are always undefined. In this study, a bioactivity-based method was developed and validated to screen lipase inhibitors and evaluate the effects of processing on the lipase inhibitory activity of TCM by ultrahigh performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry and fraction collector (UHPLC/Q-TOF-MS-FC). The results showed that both Polygonum multiflorum and processed P. multiflorum extracts had inhibitory effect against lipase with IC50 values of 38.84 μg/mL and 190.6 μg/mL, respectively. Stilbenes, phenolic acid, flavonoids, and anthraquinones were considered to be the potential lipase inhibitors. Eleven potential lipase inhibitors were simultaneously determined by UHPLC. Principal component analysis (PCA) was employed in exploring the effects of processing time on lipase inhibitory activity of P. multiflorum. Compared with conventional methods, a bioactivity-based method could quantitatively analyze lipase inhibitory activity of individual constituent and provide the total lipase inhibitory activity of the samples. The results demonstrated that the activity integrated UHPLC/Q-TOF-MS-FC method was an effective and powerful tool for screening and identifying lipase inhibitors from traditional Chinese medicines. PMID:26925151

  3. A Bioactivity-Based Method for Screening, Identification of Lipase Inhibitors, and Clarifying the Effects of Processing Time on Lipase Inhibitory Activity of Polygonum Multiflorum

    PubMed Central

    Chang, Yan-xu; Ge, Ai-hua; Jiang, Yan; Teye Azietaku, John; Li, Jin; Gao, Xiu-mei

    2016-01-01

    Traditional Chinese medicine (TCM) has been used for the treatment of many complex diseases. However, the bioactive components are always undefined. In this study, a bioactivity-based method was developed and validated to screen lipase inhibitors and evaluate the effects of processing on the lipase inhibitory activity of TCM by ultrahigh performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry and fraction collector (UHPLC/Q-TOF-MS-FC). The results showed that both Polygonum multiflorum and processed P. multiflorum extracts had inhibitory effect against lipase with IC50 values of 38.84 μg/mL and 190.6 μg/mL, respectively. Stilbenes, phenolic acid, flavonoids, and anthraquinones were considered to be the potential lipase inhibitors. Eleven potential lipase inhibitors were simultaneously determined by UHPLC. Principal component analysis (PCA) was employed in exploring the effects of processing time on lipase inhibitory activity of P. multiflorum. Compared with conventional methods, a bioactivity-based method could quantitatively analyze lipase inhibitory activity of individual constituent and provide the total lipase inhibitory activity of the samples. The results demonstrated that the activity integrated UHPLC/Q-TOF-MS-FC method was an effective and powerful tool for screening and identifying lipase inhibitors from traditional Chinese medicines. PMID:26925151

  4. Poor, Unsafe, and Overweight: The Role of Feeling Unsafe at School in Mediating the Association Among Poverty Exposure, Youth Screen Time, Physical Activity, and Weight Status

    PubMed Central

    Côté-Lussier, Carolyn; Fitzpatrick, Caroline; Séguin, Louise; Barnett, Tracie A.

    2015-01-01

    This study applied socioecological and cumulative risk exposure frameworks to test the hypotheses that 1) the experience of poverty is associated with feeling less safe at school, and 2) feeling less safe is associated with engaging in poorer weight-related behaviors, as well as an increased probability of being overweight or obese. Data were from the ongoing Québec Longitudinal Study of Child Development, initiated in 1998 with a population-based cohort of 2,120 Québec (Canada) infants 5 months of age and their parent or primary caregiver. Measures of youths' (age, 13 years) self-reported feelings of safety, screen time, physical activity, and objectively assessed not overweight/obese (70%), overweight (22%), and obese (8%) weight status were collected in 2011. Family poverty trajectory from birth was assessed by using latent growth modeling. As hypothesized, exposure to poverty was associated with feeling less safe at school and, in turn, with an increased probability of being overweight or obese. The association was most pronounced for youths who experienced chronic poverty. Compared with youths who experienced no poverty and felt unsafe, those who experienced chronic poverty and felt unsafe were nearly 18% more likely to be obese (9.2% vs. 11.2%). Although feeling unsafe was associated with screen time, screen time did not predict weight status. PMID:25921649

  5. Poor, Unsafe, and Overweight: The Role of Feeling Unsafe at School in Mediating the Association Among Poverty Exposure, Youth Screen Time, Physical Activity, and Weight Status.

    PubMed

    Côté-Lussier, Carolyn; Fitzpatrick, Caroline; Séguin, Louise; Barnett, Tracie A

    2015-07-01

    This study applied socioecological and cumulative risk exposure frameworks to test the hypotheses that 1) the experience of poverty is associated with feeling less safe at school, and 2) feeling less safe is associated with engaging in poorer weight-related behaviors, as well as an increased probability of being overweight or obese. Data were from the ongoing Québec Longitudinal Study of Child Development, initiated in 1998 with a population-based cohort of 2,120 Québec (Canada) infants 5 months of age and their parent or primary caregiver. Measures of youths' (age, 13 years) self-reported feelings of safety, screen time, physical activity, and objectively assessed not overweight/obese (70%), overweight (22%), and obese (8%) weight status were collected in 2011. Family poverty trajectory from birth was assessed by using latent growth modeling. As hypothesized, exposure to poverty was associated with feeling less safe at school and, in turn, with an increased probability of being overweight or obese. The association was most pronounced for youths who experienced chronic poverty. Compared with youths who experienced no poverty and felt unsafe, those who experienced chronic poverty and felt unsafe were nearly 18% more likely to be obese (9.2% vs. 11.2%). Although feeling unsafe was associated with screen time, screen time did not predict weight status. PMID:25921649

  6. Automation of antimicrobial activity screening.

    PubMed

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

    2016-03-01

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

  7. Development of Neh2-luciferase reporter and its application for high throughput screening and real-time monitoring of Nrf2 activators.

    PubMed

    Smirnova, Natalya A; Haskew-Layton, Renee E; Basso, Manuela; Hushpulian, Dmitry M; Payappilly, Jimmy B; Speer, Rachel E; Ahn, Young-Hoon; Rakhman, Ilay; Cole, Philip A; Pinto, John T; Ratan, Rajiv R; Gazaryan, Irina G

    2011-06-24

    The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2, we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). We show that Neh2 domain is sufficient for recognition, ubiquitination, and proteasomal degradation of Neh2-luciferase fusion protein. The Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time course of reporter activation. The reporter was used to screen the Spectrum library of 2000 biologically active compounds to identify activators of Nrf2. The most robust and yet nontoxic Nrf2 activators found--nordihydroguaiaretic acid, fisetin, and gedunin--induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism. PMID:21700211

  8. Development of Neh2-Luciferase Reporter and Its Application for High Throughput Screening and Real-Time Monitoring of Nrf2 Activators

    PubMed Central

    Smirnova, Natalya A.; Haskew-Layton, Renee E.; Basso, Manuela; Hushpulian, Dmitry M.; Payappilly, Jimmy B.; Speer, Rachel E.; Ahn, Young-Hoon; Rakhman, Ilay; Cole, Philip A.; Pinto, John T.; Ratan, Rajiv R.; Gazaryan, Irina G.

    2011-01-01

    SUMMARY The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2, we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). We show that Neh2 domain is sufficient for recognition, ubiquitination, and proteasomal degradation of Neh2-luciferase fusion protein. The Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time course of reporter activation. The reporter was used to screen the Spectrum library of 2000 biologically active compounds to identify activators of Nrf2. The most robust and yet nontoxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin—induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism. PMID:21700211

  9. Prevalence of excessive screen time and associated factors in adolescents

    PubMed Central

    de Lucena, Joana Marcela Sales; Cheng, Luanna Alexandra; Cavalcante, Thaísa Leite Mafaldo; da Silva, Vanessa Araújo; de Farias, José Cazuza

    2015-01-01

    Objective: To determine the prevalence of excessive screen time and to analyze associated factors among adolescents. Methods: This was a cross-sectional school-based epidemiological study with 2874 high school adolescents with age 14-19 years (57.8% female) from public and private schools in the city of João Pessoa, PB, Northeast Brazil. Excessive screen time was defined as watching television and playing video games or using the computer for more than 2 h/day. The associated factors analyzed were: sociodemographic (gender, age, economic class, and skin color), physical activity and nutritional status of adolescents. Results: The prevalence of excessive screen time was 79.5% (95%CI 78.1-81.1) and it was higher in males (84.3%) compared to females (76.1%; p<0.001). In multivariate analysis, adolescent males, those aged 14-15 year old and the highest economic class had higher chances of exposure to excessive screen time. The level of physical activity and nutritional status of adolescents were not associated with excessive screen time. Conclusions: The prevalence of excessive screen time was high and varied according to sociodemographic characteristics of adolescents. It is necessary to develop interventions to reduce the excessive screen time among adolescents, particularly in subgroups with higher exposure. PMID:26298661

  10. Insights and implications for health departments from the evaluation of New York City's regulations on nutrition, physical activity, and screen time in child care centers.

    PubMed

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

    2014-01-01

    In 2006, the New York City Department of Health and Mental Hygiene, seeking to address the epidemic of childhood obesity, issued new regulations on beverages, physical activity, and screen time in group child care centers. An evaluation was conducted to identify characteristics of New York City child care centers that have implemented these regulations and to examine how varying degrees of implementation affected children's behaviors. This article discusses results of this evaluation and how findings can be useful for other public health agencies. Knowing the characteristics of centers that are more likely to comply can help other jurisdictions identify centers that may need additional support and training. Results indicated that compliance may improve when rules established by governing agencies, national standards, and local regulatory bodies are complementary or additive. Therefore, the establishment of clear standards for obesity prevention for child care providers can be a significant public health achievement. PMID:25321629

  11. Gold nanoclusters-Cu(2+) ensemble-based fluorescence turn-on and real-time assay for acetylcholinesterase activity and inhibitor screening.

    PubMed

    Sun, Jian; Yang, Xiurong

    2015-12-15

    Based on the specific binding of Cu(2+) ions to the 11-mercaptoundecanoic acid (11-MUA)-protected AuNCs with intense orange-red emission, we have proposed and constructed a novel fluorescent nanomaterials-metal ions ensemble at a nonfluorescence off-state. Subsequently, an AuNCs@11-MUA-Cu(2+) ensemble-based fluorescent chemosensor, which is amenable to convenient, sensitive, selective, turn-on and real-time assay of acetylcholinesterase (AChE), could be developed by using acetylthiocholine (ATCh) as the substrate. Herein, the sensing ensemble solution exhibits a marvelous fluorescent enhancement in the presence of AChE and ATCh, where AChE hydrolyzes its active substrate ATCh into thiocholine (TCh), and then TCh captures Cu(2+) from the ensemble, accompanied by the conversion from fluorescence off-state to on-state of the AuNCs. The AChE activity could be detected less than 0.05 mU/mL within a good linear range from 0.05 to 2.5 mU/mL. Our proposed fluorescence assay can be utilized to evaluate the AChE activity quantitatively in real biological sample, and furthermore to screen the inhibitor of AChE. As far as we know, the present study has reported the first analytical proposal for sensing AChE activity in real time by using a fluorescent nanomaterials-Cu(2+) ensemble or focusing on the Cu(2+)-triggered fluorescence quenching/recovery. This strategy paves a new avenue for exploring the biosensing applications of fluorescent AuNCs, and presents the prospect of AuNCs@11-MUA-Cu(2+) ensemble as versatile enzyme activity assay platforms by means of other appropriate substrates/analytes. PMID:26141104

  12. High-content screening imaging and real-time cellular impedance monitoring for the assessment of chemical's bio-activation with regards hepatotoxicity.

    PubMed

    Peyre, Ludovic; de Sousa, Georges; Barcellini-Couget, Sylvie; Luzy, Anne-Pascale; Zucchini-Pascal, Nathalie; Rahmani, Roger

    2015-10-01

    Testing hepatotoxicity is a crucial step in the development and toxicological assessment of drugs and chemicals. Bio-activation can lead to the formation of metabolites which may present toxicity for the organism. Classical cytotoxic tests are not always appropriate and are often insufficient, particularly when non metabolically-competent cells are used as the model system, leading to false-positive or false-negative results. We tested over 24 h the effects of eight reference compounds on two different cell models: primary cultures of rat hepatocytes and FAO hepatoma cells that lack metabolic properties. We performed inter-assay validation between three classical cytotoxicity assays and real-time cell impedance data. We then complemented these experiments with high-content screening (HCS) to determine the cell function disorders responsible for the observed effects. Among the different assays used, the neutral red test seemed to be well suited to our two cell models, coupled with real-time cellular impedance which proved useful in the detection of bio-activation. Indeed, impedance monitoring showed a high sensitivity with interesting curve profiles yet seemed unsuitable for evaluation of viability on primary culture. Finally, HCS in the evaluation of hepatotoxicity is likely to become an essential tool for use in parallel to a classical cytotoxic assay in the assessment of drugs and environmental chemicals. PMID:26239606

  13. Parent-Child Relationship of Pedometer-Assessed Physical Activity and Proxy-Reported Screen Time in Czech Families with Preschoolers

    PubMed Central

    Sigmund, Erik; Badura, Petr; Vokacova, Jana; Sigmundová, Dagmar

    2016-01-01

    This study focuses on determining the relationship between parents’ step count (SC) and screen time (ST) and children’s SC and ST on weekdays and at weekends. The participants (278 parents aged 30–45 and their 194 children aged 4–7) were recruited from 10 randomly selected Czech kindergartens. The participants recorded SC and ST duration over a week-long monitoring (≥8 h/day) during September–October 2014 and April–May 2015. The associations between parents’ SC and ST and children’s SC and ST were estimated using general linear regression for weekdays and weekends. Each 2500 SC increase in mothers’/fathers’ daily SC at weekdays (weekends) was associated with an extra 1143/903 (928/753) daily SC in children. Each 60 min of ST increase in mothers’/fathers’ ST at weekdays (weekends) was associated with an extra 7.6/7.6 (16.8/13.0) min of child daily ST. An increase of 2500 mothers’ daily SC was associated with reduction of 2.5 (7.5) min of ST in children at weekdays (weekends). This study reveals a significant relationship between parent-child SC/day, parent-child ST/day, and mothers’ ST and children’s SC at weekends. Weekend days seem to provide a suitable space for the promotion of joint physical activity in parents and their pre-schoolers. PMID:27455293

  14. Active Case Finding of Pulmonary Tuberculosis through Screening of Respiratory Symptomatics Using Sputum Microscopy: Is It Time to Change the Paradigm?

    PubMed Central

    del Portillo-Mustieles, Eva Carolina; Laniado-Laborín, Rafael

    2013-01-01

    Background. One of the main strategies for the early detection of pulmonary tuberculosis (PTB) is through the screening of individuals with symptoms compatible with PTB. Although this is programmatic strategy for active case finding, its yield is not well known. Objective. To determine the yield of pulmonary tuberculosis active case finding through the screening of respiratory symptomatic (RS) patients at a general hospital. Methods. RS patients were defined as subjects complaining of cough and/or sputum for a period of 2 or more weeks. Outpatients and their companions were approached while they waited in the outpatient care areas of the hospital to detect RS. Two samples from different days or 2 samples taken 2 hours apart on the same day were collected. Results. 122 RS patients were identified. Fifty-seven patients (46.7%) had at least one sputum sample analyzed. Three patients presented a positive smear and 2 were culture positive; neither had upper airway symptoms. None of the patients with productive cough and upper airway symptoms had a positive smear (P = 0.07). Only 19 (33.3%) returned to the laboratory to retrieve their results. Conclusion. Current strategy to screen RS patients based only on clinical data has a low compliance. Specific strategies to increase compliance (removal of barriers, incentives, etc.) should be implemented. PMID:23533747

  15. Low Physical Activity and High Screen Time Can Increase the Risks of Mental Health Problems and Poor Sleep Quality among Chinese College Students

    PubMed Central

    Zhang, Yukun; Zhang, Shichen; Tao, Fangbiao

    2015-01-01

    Objective To test the independent and interactive associations of physical activity (PA) and screen time (ST) with self-reported mental health and sleep quality among Chinese college students. Method Data were collected in October, 2013. The gender, age, residential background, body mass index (BMI), perceived family economy and perceived study burden were obtained from a total of 4747 college students (41.6% males and 58.4% females). The outcomes were self-reported PA status, ST, anxiety, depression, psychopathological symptoms and sleep quality. Analyses were conducted with logistic regression models. Results Overall, 16.3%, 15.9% and 17.3% of the students had psychological problems, such as anxiety, depression and psychopathological symptoms, respectively. The prevalence of poor sleep quality was 9.8%. High ST was significantly positively associated with anxiety (OR=1.38, 95%CI: 1.15-1.65), depression (OR=1.76, 95%CI: 1.47-2.09), psychopathological symptoms (OR=1.69, 95%CI: 1.43-2.01) and poor sleep quality (OR=1.32, 95%CI: 1.06-1.65). High PA was insignificantly negatively associated with anxiety, depression, psychopathological symptoms and poor sleep. Low PA and high ST were independently and interactively associated with increased risks of mental health problems and poor sleep quality (p<0.05 for all). Conclusion Interventions are needed to reduce ST and increase PA in the lifestyles of young people. Future research should develop and measure the impacts of interventions and their potential consequences on sleep, health, and well being. PMID:25786030

  16. Temporal Trends in Overweight and Obesity, Physical Activity and Screen Time among Czech Adolescents from 2002 to 2014: A National Health Behaviour in School-Aged Children Study

    PubMed Central

    Sigmund, Erik; Sigmundová, Dagmar; Badura, Petr; Kalman, Michal; Hamrik, Zdenek; Pavelka, Jan

    2015-01-01

    This study examines trends in overweight and obesity, physical activity (PA) and screen time (ST) among Czech adolescents over a recent 12-year study period. Nationally representative samples consisted of 19,940 adolescents (9760 boys and 10,180 girls) aged 10.5–16.5 years from the Czech Health Behaviour in School-aged Children (HBSC) questionnaire-based surveys conducted in 2002, 2006, 2010 and 2014. Trends in the prevalence of overweight/obesity, meeting the recommendations for moderate-to-vigorous PA (MVPA) (≥60 min per day of MVPA) and excessive ST (>2 h per day) were estimated using logistic regression. Significant increases (p < 0.001) in the prevalence of overweight/obesity between the years 2002 and 2014 were evident for both adolescent boys (18.3%2002–24.8%2014) and girls (8.3%2002–11.9%2014). Compared to 2002, in 2014 significant decreases (p < 0.001) in meeting MVPA recommendations were observed among boys (32.2%2002–25.6%2014) and girls (23.2%2002–19.2%2014). Moreover, in boys we observed significant increases (p < 0.001) in excessive ST on weekdays (75.1%2002–88.8%2014), as well as on weekends (78.3%2002–91.9%2014) between the years 2002 and 2014. Increases in overweight/obesity with concomitant decreases in PA provide evidence in support of the current and upcoming efforts of government and commercial organizations in implementing interventions aimed at reducing excessive body weight among Czech adolescents. PMID:26393638

  17. Screening Actinomycetes for Extracellular Peroxidase Activity

    PubMed Central

    Mercer, D. K.; Iqbal, M.; Miller, P.; McCarthy, A. J.

    1996-01-01

    A diverse collection of actinomycete strains were screened for production of extracellular peroxidase activity by adapting a chemiluminescence analysis system developed for horseradish peroxidase-based enzyme-linked immunosorbent assay. Extracellular peroxidase activity was found to be common but quantitatively variable, and this rapid and sensitive screening system permitted identification of a small group of high-producing strains. A range of spectrophotometric assays were compared for the measurement of peroxidase activity in concentrated culture supernatants of two selected thermophilic streptomycetes. Of these, the peroxide-dependent oxidation of 2,4-dichlorophenol was identified as the most robust and reproducible assay for quantitative studies. PMID:16535344

  18. Real-time investigation of human topoisomerase I reaction kinetics using an optical sensor: a fast method for drug screening and determination of active enzyme concentrations

    NASA Astrophysics Data System (ADS)

    Kristoffersen, Emil L.; Jørgensen, Line A.; Franch, Oskar; Etzerodt, Michael; Frøhlich, Rikke; Bjergbæk, Lotte; Stougaard, Magnus; Ho, Yi-Ping; Knudsen, Birgitta R.

    2015-05-01

    Human DNA topoisomerase I (hTopI) is a nuclear enzyme that catalyzes relaxation of super helical tension that arises in the genome during essential DNA metabolic processes. This is accomplished through a common reaction mechanism shared among the type IB topoisomerase enzymes, including eukaryotic and poxvirus topoisomerase I. The mechanism of hTopI is specifically targeted in cancer treatment using camptothecin derivatives. These drugs convert the hTopI activity into a cellular poison, and hence the cytotoxic effects of camptothecin derivatives correlate with the hTopI activity. Therefore, fast and reliable techniques for high throughput measurements of hTopI activity are of high clinical interest. Here we demonstrate potential applications of a fluorophore-quencher based DNA sensor designed for measurement of hTopI cleavage-ligation activities, which are the catalytic steps affected by camptothecin. The kinetic analysis of the hTopI reaction with the DNA sensor exhibits a characteristic burst profile. This is the result of a two-step ping-pong reaction mechanism, where a fast first reaction, the one creating the signal, is followed by a slower second reaction necessary for completion of the catalytic cycle. Hence, the burst profile holds information about two reactions in the enzymatic mechanism. Moreover, it allows the amount of active enzyme in the reaction to be determined. The presented results pave the way for future high throughput drug screening and the potential of measuring active hTopI concentrations in clinical samples for individualized treatment.Human DNA topoisomerase I (hTopI) is a nuclear enzyme that catalyzes relaxation of super helical tension that arises in the genome during essential DNA metabolic processes. This is accomplished through a common reaction mechanism shared among the type IB topoisomerase enzymes, including eukaryotic and poxvirus topoisomerase I. The mechanism of hTopI is specifically targeted in cancer treatment using

  19. 'Life in the age of screens': parent perspectives on a 24-h no screen-time challenge.

    PubMed

    Peláez, Sandra; Alexander, Stephanie; Roberge, Jean-Baptiste; Henderson, Melanie; Bigras, Jean-Luc; Barnett, Tracie A

    2016-08-01

    Screens have become ubiquitous in modern society. Their use frequently underlies sedentary behaviour, a well-established determinant of obesity. As part of a family oriented clinic offering a 2-year lifestyle program for obese children and youth, we explored parents' experiences with a 24-h no screen-time challenge, an intervention designed to raise awareness of screen-time habits and to help families develop strategies to limit their use. In total, 15 parents representing 13 families participated. A focus group with nine parents and six phone interviews with those who could not join in person were conducted. Interviews were transcribed verbatim and analysed qualitatively. Key elements to successful completion of the 24-h no screen-time challenge emerged, namely: clear rules about permitted activities during the 24-h period; togetherness, i.e. involving all family members in the challenge; and busyness, i.e. planning a full schedule in order to avoid idleness and preclude the temptation to use screens. Our findings suggest that practitioners aiming to increase awareness of screen-time or to limit their use may be more likely to succeed if they include all family members, offer concrete alternatives to screen-based activities and provide tailored strategies to manage discretionary time. PMID:27242271

  20. Sport participation, screen time, and personality trait development during childhood.

    PubMed

    Allen, Mark S; Vella, Stewart A; Laborde, Sylvain

    2015-09-01

    This investigation explored the contribution of extracurricular sport and screen time viewing (television viewing and electronic gaming) to personality trait stability and change during childhood. Two independent samples of 3,956 young children (age 6) and 3,862 older children (age 10) were taken from the Longitudinal Study of Australian Children. Parent-reported child sport participation, screen time, and personality traits were measured at baseline and again 24 months later. Young children who were more active recorded more of a decrease in introversion, less of a decrease in persistence, and less of an increase in reactivity, than those who were less active. Older children who were more active recorded less of an increase in introversion and more of an increase in persistence than those who were less active. In addition, young children who continued participation in extracurricular sport had greater intra-individual stability of personality for introversion. These finding suggest that an active lifestyle might help to facilitate desirable personality trait stability and change during childhood. PMID:26259042

  1. A high-throughput screening-compatible homogeneous time-resolved fluorescence assay measuring the glycohydrolase activity of human poly(ADP-ribose) glycohydrolase.

    PubMed

    Stowell, Alexandra I J; James, Dominic I; Waddell, Ian D; Bennett, Neil; Truman, Caroline; Hardern, Ian M; Ogilvie, Donald J

    2016-06-15

    Poly(ADP-ribose) (PAR) polymers are transient post-translational modifications, and their formation is catalyzed by poly(ADP-ribose) polymerase (PARP) enzymes. A number of PARP inhibitors are in advanced clinical development for BRCA-mutated breast cancer, and olaparib has recently been approved for BRCA-mutant ovarian cancer; however, there has already been evidence of developed resistance mechanisms. Poly(ADP-ribose) glycohydrolase (PARG) catalyzes the hydrolysis of the endo- and exo-glycosidic bonds within the PAR polymers. As an alternative strategy, PARG is a potentially attractive therapeutic target. There is only one PARG gene, compared with 17 known PARP family members, and therefore a PARG inhibitor may have wider application with fewer compensatory mechanisms. Prior to the initiation of this project, there were no known existing cell-permeable small molecule PARG inhibitors for use as tool compounds to assess these hypotheses and no suitable high-throughput screening (HTS)-compatible biochemical assays available to identify start points for a drug discovery project. The development of this newly described high-throughput homogeneous time-resolved fluorescence (HTRF) assay has allowed HTS to proceed and, from this, the identification and advancement of multiple validated series of tool compounds for PARG inhibition. PMID:27036617

  2. Impact of e-Discipline on Children's Screen Time

    PubMed Central

    Rupert, Maya Samaha

    2015-01-01

    Abstract With rapid technological advancement, the prevalence and undesirable effects of excess screen time on children have become a mounting issue worldwide. There are many studies investigating the phenomenon's impact on society (e.g., behavioral, academic, health), but studies that uncover the causes and factors that increase the odds of children's excess screen time are limited. To this end, this study introduces the term “e-discipline” to refer to systematic practices that use screen devices as discipline tools. As such, the aim of this study is to investigate the association between e-discipline and children's screen time by gender. Analysis was performed on 3,141 children aged 7–11 years old. Bivariate logistic regression models were used to calculate the odds of exceeding the American Academy of Pediatrics guidelines of 2 hours of screen time per day by boys and girls whose parents practice e-discipline. The results showed that children whose parents used screen devices as discipline tools had significantly more screen time compared to children whose parents did not. Furthermore, no statistically significant gender differences were found in the odds of exceeding the recommended screen time under e-discipline. Recommendations stemming from all the results are discussed. PMID:26075921

  3. Associations between dietary patterns and screen time among Korean adolescents

    PubMed Central

    Lee, Jae Yeon; Jun, Nuri

    2013-01-01

    Data are limited on the association between dietary patterns and screen time among Korean adolescents. The present study identified dietary patterns of 691 adolescents, aged 13-18 years, who had participated in the Third Korean National Health and Nutrition Examination Survey (KNHANES III) and analyzed their associations with screen time. Screen time was defined as the time spent watching TV, using a computer, or playing video games was calculated as a sum of all these times. Dietary patterns and their factor scores were derived from a food frequency questionnaire using the factor analysis method. To analyze the association between dietary patterns and screen time, we conducted multiple linear regression analysis. We also performed multiple logistic regression analysis to estimate odds ratios (OR) of excessive screen time (2 hours or longer per day) and 95% confidence intervals (CI). We identified 2 dietary patterns labeled "the Korean healthy dietary pattern" and "the Western diet and fast foods pattern". The former included mixed grains, legumes, potatoes, red meat, eggs, fish, dairy products, fruits, vegetables, seaweeds, and mushrooms, whereas the latter included noodles, bread, red meat, poultry, fast foods, snack, and soft drinks. After controlling for potential confounding factors, factor scores for the Korean healthy dietary pattern were inversely associated (P-value for trend < 0.01) and those for the Western diet and fast foods pattern were positively associated with the screen time (P-value for trend < 0.01). Adolescents in the top tertile of the scores for the Korean healthy dietary pattern had a multivariable-adjusted OR [95% CI] of 0.44 (0.25-0.75) for excessive screen time compared with those in the lowest tertile. On the basis of these findings, adolescents who have excessive screen time may need to be encouraged to consume a more healthy diet. PMID:23964322

  4. Screen time and adiposity in adolescents in Mexico

    PubMed Central

    Lajous, Martín; Chavarro, Jorge; Peterson, Karen E; Hernández-Prado, Bernardo; Cruz-Valdéz, Aurelio; Hernández-Ávila, Mauricio; Lazcano-Ponce, Eduardo

    2014-01-01

    Objective To assess the association of time spent viewing television, videos and videogames with measures of fat mass [body mass index (BMI)] and distribution [triceps and subscapular skin folds (TSF, SSF)]. Design Cross-sectional validated survey, self-administered to students to assess screen time (TV, videos and videogames) and lifestyle variables. Trained personnel obtained anthropometry. The association of screen time with fat mass and distribution, stratified by sex, was modeled with multivariable linear regression, adjusting for potential confounders and correlation of observations within schools. Subjects and setting 3519 males and 5613 females aged 11 to 18 years attending urban and rural schools in the State of Morelos, Mexico Results In males, ≥5 hr/day compared with < 2 hr/day of screen time, was significantly associated with a 0.13 (95%CI 0.04, 0.23) higher BMI z score, 0.73 mm (95% CI 0.24, 1.22) higher SSF and 1.08 mm (95% CI 0.36, 1.81) higher TSF. The positive association of screen time with SSF was strongest in males 11–12 yr. Sexual maturity appeared to modify the association in females; a positive between screen time and SSF was observed in those who had not undergone menarche (p-trend 0.04) but not among sexually mature females (p-trend 0.75). Conclusion Screen time is associated with fat mass and distribution among adolescent males in Mexico. Maturational tempo appears to affect the relationship of screen time with adiposity in boys and girls. Findings suggest obesity preventive interventions in the Mexican context should explore strategies to reduce screen time among youth in early adolescence. PMID:19232154

  5. Beyond Screen Time: Assessing Recreational Sedentary Behavior among Adolescent Girls

    PubMed Central

    Bauer, Katherine W.; Friend, Sarah; Graham, Daniel J.; Neumark-Sztainer, Dianne

    2012-01-01

    Most studies of sedentary behavior have focused on television use or screen time. This study aims to examine adolescent girls' participation in a variety of recreational sedentary behaviors (e.g., talking on the phone and hanging around), and their association with physical activity (PA), dietary behaviors, and body mass index. Data were from a sample of 283 adolescent girls. Recreational sedentary behavior, PA, and dietary behaviors were self-reported, and girls' height and weight were measured. Over 95% of girls engaged in at least one recreational sedentary behavior during the recall period. Watching television and hanging around were the most common behaviors. Watching television, using the Internet, and hanging around were associated with less PA; watching television, hanging around, and talking on the phone were associated with less healthful dietary behaviors. No associations were found with body mass index. Interventions may benefit from capitalizing on and intervening upon girls' common recreational sedentary behaviors. PMID:22013514

  6. A systematic review and meta-analysis of screen time behaviour among North American indigenous populations.

    PubMed

    Foulds, H J A; Rodgers, C D; Duncan, V; Ferguson, L J

    2016-05-01

    Screen time (computer, television, video game and smartphone/tablet activity) is associated with increased obesity and other health risks. This systematic review evaluates screen time among North American Indigenous populations and compares it with that of North American Europeans. Electronic databases (e.g. MEDLINE and EMBASE) were searched, and citations cross-referenced. Included articles reported screen time among First Nations/American Indians, Métis, Inuit/Alaskan Natives or Native Hawaiians. From 788 citations evaluated, 40 identified articles report television, video game, computer and/or overall screen time. Overall screen time was 3.65 ± 1.26 h day(-1) (n = 2,242, 8 articles) among Indigenous children/youth and 3.61 ± 2.95 h day(-1) (n = 155, 1 article) among adults. Among children/youth, 66.0% (n = 11 256, 9 articles) reported less than 2 h day(-1) of television screen time, while only 52.8% (n = 2,458, 1 article) of adults reported this volume. Screen time was generally greater among male population, youth, First Nations/American Indians and overweight/obese individuals. Indigenous children/youth reported greater overall screen time than North American Europeans (4.81 ± 2.84 h day(-1) , n = 1,182 vs. 3.40 ± 2.81 h day(-1) , n = 2,785; 3 articles; p < 0.0001). Screen time is common among North American Indigenous populations. Further research evaluating interventions to reduce screen time and chronic disease risks is required. PMID:26990323

  7. Projection type transparent 3D display using active screen

    NASA Astrophysics Data System (ADS)

    Kamoshita, Hiroki; Yendo, Tomohiro

    2015-05-01

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

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

    PubMed

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

    2015-10-01

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

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

    PubMed Central

    Dobler, Claudia Caroline

    2016-01-01

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

  10. Bedroom media, sedentary time and screen-time in children: a longitudinal analysis

    PubMed Central

    2013-01-01

    Background Having electronic media in the bedroom is cross-sectionally associated with greater screen-time in children, but few longitudinal studies exist. The aim of this study was to describe longitudinal patterns of ownership and examine cross-sectional and longitudinal associations of bedroom media with children’s sedentary behaviour. Methods Data are from the Sport, Physical activity and Eating behaviour: Environmental Determinants in Young people (SPEEDY) study, collected at 3 time-points: baseline (2007, T0; age 10.3 ± 0.3 years), 1-year (T1y) and 4-year (T4y) follow-up. For each assessment, 1512 (44.9% male), 715 (41.0% male), and 319 (48.3% male) participants provided valid accelerometer data. Outcome variables were accelerometer-assessed sedentary time and self-reported screen-time. The presence of a television or computer in the bedroom was self-reported by participants and a combined bedroom media score calculated as the sum of such items. Cross-sectional and longitudinal associations between bedroom media and each outcome were examined using multi-level linear regression. Results Bedroom TV ownership fell from 70.9% at T0 to 42.5% at T4y. Having a TV in the bedroom (beta; 95% CI*100, T0: -1.17; -1.88, -0.46. T1y: -1.68; -2.67, -0.70) and combined bedroom media (T0: -0.76; -1.26, -0.27. T1y: -0.79; -1.51, -0.07) were negatively associated with objectively measured weekly sedentary time at T0 and T1y. Having a computer in the bedroom (beta; 95% CI, T0: 0.15; 0.02, 0.29. T4y: 0.35; 0.10, 0.60) and combined bedroom media (T0: 0.09: 0.01, 0.18. T4y: 0.20; 0.05, 0.34) were positively associated with screen-time at T0 and T4y. Relative to participants without a computer throughout the study, children that had a computer in their bedroom at T0 but not at T4y (beta; 95% CI for change in screen-time: -8.02; -12.75, -3.29) reported smaller increases in screen-time. Conclusions The bedroom media environment changes with age and exhibits a complex

  11. Does patient time spent viewing computer-tailored colorectal cancer screening materials predict patient-reported discussion of screening with providers?

    PubMed

    Sanders, Mechelle; Fiscella, Kevin; Veazie, Peter; Dolan, James G; Jerant, Anthony

    2016-08-01

    The main aim is to examine whether patients' viewing time on information about colorectal cancer (CRC) screening before a primary care physician (PCP) visit is associated with discussion of screening options during the visit. We analyzed data from a multi-center randomized controlled trial of a tailored interactive multimedia computer program (IMCP) to activate patients to undergo CRC screening, deployed in primary care offices immediately before a visit. We employed usage time information stored in the IMCP to examine the association of patient time spent using the program with patient-reported discussion of screening during the visit, adjusting for previous CRC screening recommendation and reading speed.On average, patients spent 33 minutes on the program. In adjusted analyses, 30 minutes spent using the program was associated with a 41% increase in the odds of the patient having a discussion with their PCP (1.04, 1.59, 95% CI). In a separate analysis of the tailoring modules; the modules encouraging adherence to the tailored screening recommendation and discussion with the patient's PCP yielded significant results. Other predictors of screening discussion included better self-reported physical health and increased patient activation. Time spent on the program predicted greater patient-physician discussion of screening during a linked visit.Usage time information gathered automatically by IMCPs offers promise for objectively assessing patient engagement around a topic and predicting likelihood of discussion between patients and their clinician. PMID:27343254

  12. Family structure as a predictor of screen time among youth.

    PubMed

    McMillan, Rachel; McIsaac, Michael; Janssen, Ian

    2015-01-01

    The family plays a central role in the development of health-related behaviors among youth. The objective of this study was to determine whether non-traditional parental structure and shared custody arrangements predict how much time youth spend watching television, using a computer recreationally, and playing video games. Participants were a nationally representative sample of Canadian youth (N = 26,068) in grades 6-10 who participated in the 2009/10 Health Behaviour in School-aged Children Survey. Screen time in youth from single parent and reconstituted families, with or without regular visitation with their non-residential parent, was compared to that of youth from traditional dual-parent families. Multiple imputation was used to account for missing data. After multiple imputation, the relative odds of being in the highest television, computer use, video game, and total screen time quartiles were not different in boys and girls from non-traditional families by comparison to boys and girls from traditional dual-parent families. In conclusion, parental structure and child custody arrangements did not have a meaningful impact on screen time among youth. PMID:26137429

  13. Family structure as a predictor of screen time among youth

    PubMed Central

    McMillan, Rachel; McIsaac, Michael

    2015-01-01

    The family plays a central role in the development of health-related behaviors among youth. The objective of this study was to determine whether non-traditional parental structure and shared custody arrangements predict how much time youth spend watching television, using a computer recreationally, and playing video games. Participants were a nationally representative sample of Canadian youth (N = 26,068) in grades 6–10 who participated in the 2009/10 Health Behaviour in School-aged Children Survey. Screen time in youth from single parent and reconstituted families, with or without regular visitation with their non-residential parent, was compared to that of youth from traditional dual-parent families. Multiple imputation was used to account for missing data. After multiple imputation, the relative odds of being in the highest television, computer use, video game, and total screen time quartiles were not different in boys and girls from non-traditional families by comparison to boys and girls from traditional dual-parent families. In conclusion, parental structure and child custody arrangements did not have a meaningful impact on screen time among youth. PMID:26137429

  14. Screen time, weight status and the self-concept of physical attractiveness in adolescents.

    PubMed

    Suchert, Vivien; Hanewinkel, Reiner; Isensee, Barbara

    2016-04-01

    Adolescents in modern societies spend about 3 h per day in front of small recreational screens. The present study aims at investigating the relationships between screen time and different indicators of overweight. In addition, associations with the self-concept of physical attractiveness and perceived weight status will be examined. In a total sample of 1228 students (47.5% girls) aged 12-17 years (M = 13.74, SD = 0.68) cross-sectional associations were determined by conducting multiple linear regression analyses. Screen time showed a significant positive dose-response relationship with body mass index percentile, waist circumference, body fat, waist-to-height-ratio, and a negative association with self-concept of physical attractiveness independent of age, gender and moderate to vigorous physical activity. Thus, screen time seems to be associated with adolescent overweight, abdominal obesity, and body dissatisfaction. Reducing adolescents' screen time could be a promising approach for primary prevention of obesity and for the promotion of a positive physical self-concept. PMID:26854729

  15. Baby unplugged: a novel, market-based approach to reducing screen time and promoting healthy alternatives.

    PubMed

    Hutton, John S

    2013-01-01

    The issue of electronic media use by young children is increasingly important in pediatrics, a major risk factor for numerous chronic conditions. Despite guidelines in place since 1999, screen time is on the rise, aided by new formats removing practically all barriers of use. Key drivers are technological allure, confusion about developmental readiness, and perception of educational value, fueled by potent marketing. This article describes the development of Baby Unplugged, a series of children's board books celebrating "old-school," screen-free childhood. Written by a pediatrician who also owns a children's bookstore, the books were inspired and informed by advocacy projects in the areas of media use and early literacy as a pediatric resident. They reinforce AAP Electronic Media Guidelines, notably discouraging screen-based media under 2 years old, largely by encouraging healthy, fun alternatives. Examples include Pets, Book, and Yard. Multi-sensorial exploration and parent-child engagement are emphasized in a non-prescriptive way, featuring gender and ethnic diversity and activities that are accessible and inexpensive. The author describes challenges faced by pediatricians providing anticipatory guidance for media use, given limited time and resources and the perception that we are out of touch. This is heightened by oft-deceptive marketing of screen-based products more likely to be perceived as "cool." Reach Out and Read is cited as an example of a successful, "cool" intervention, though limited to select populations. Baby Unplugged takes advocacy to the marketplace, where the screen time battle is being lost. PMID:23172903

  16. Influencing factors of screen time in preschool children: an exploration of parents' perceptions through focus groups in six European countries.

    PubMed

    De Decker, E; De Craemer, M; De Bourdeaudhuij, I; Wijndaele, K; Duvinage, K; Koletzko, B; Grammatikaki, E; Iotova, V; Usheva, N; Fernández-Alvira, J M; Zych, K; Manios, Y; Cardon, G

    2012-03-01

    Preschoolers already spend significant proportions of their waking hours being sedentary. Screen time (i.e. television/DVD viewing and computer use) has been negatively associated with several health outcomes but interventions aiming to reduce preschoolers' sedentary behaviour are scarce. This study aimed to explore parents' perceptions of their preschool children's screen time. One hundred twenty-two parents of low and medium-high socioeconomic status from six European countries with children between 4 and 6 years old were involved in 24 focus groups. Following a qualitative content analysis, the available information and key findings were centrally analysed. Results showed that children tend to like watching television (TV) and most parents do not express worries about their children's TV viewing time. Education is considered to be the main benefit of watching TV and in general, parents only have informal rules about TV viewing. Computer and active games use are less frequent compared with TV viewing. No univocal results are found about the influence of siblings or friends on children's screen time. Weather conditions and parental habits at home are the most important factors influencing children's screen time. Alternatives for screen activities and information on how to set rules for screen time should be provided to parents to assist them in decreasing their preschool children's screen time. PMID:22309066

  17. A Real-Time Screening Alert Improves Patient Recruitment Efficiency

    PubMed Central

    Weng, Chunhua; Batres, Candido; Borda, Tomas; Weiskopf, Nicole G.; Wilcox, Adam B.; Bigger, J Thomas; Davidson, Karina W.

    2011-01-01

    The scarcity of cost-effective patient identification methods represents a significant barrier to clinical research. Research recruitment alerts have been designed to facilitate physician referrals but limited support is available to clinical researchers. We conducted a retrospective data analysis to evaluate the efficacy of a real-time patient identification alert delivered to clinical research coordinators recruiting for a clinical prospective cohort study. Data from log analysis and informal interviews with coordinators were triangulated. Over a 12-month period, 11,295 were screened electronically, 1,449 were interviewed, and 282 were enrolled. The enrollment rates for the alert and two other conventional methods were 4.65%, 2.01%, and 1.34% respectively. A taxonomy of eligibility status was proposed to precisely categorize research patients. Practical ineligibility factors were identified and their correlation with age and gender were analyzed. We conclude that the automatic prescreening alert improves screening efficiency and is an effective aid to clinical research coordinators. PMID:22195213

  18. Screening wastewater for toxicity to activated sludge

    SciTech Connect

    Schneider, C.G.

    1987-01-01

    Several toxicity tests were compared to define their utility for prediction of toxicity to activated sludge. The tests included: (1) oxygen uptake rates in batch tests with activated sludge, (2) adenosine triphosphate (ATP) measurements in the same batch tests, (3) Warburg respirometer studies with activated sludge, and (4) a luminescent bacteria test (Microtox/sup TM/). An evaluation of the toxicity tests was made with several toxicants; nickel (II), mercury (II), 2,4-dichlorophenol (DCP) and 4,6-dinitro-o-cresol (DNOC). Because of differences in toxic mechanism, some of the toxicants produced greater toxic effects in some tests than in other tests. The ATP levels decreased significant when uncouplers of oxidative phosphorylation were studied (DCP and DNOC). Several procedures for measuring ATP were investigated and were found to be unsatisfactory when applied to activated sludge. A new method for extraction of ATP, which incorporated a sonic bath and trichloroacetic acid, was developed. The improved ATP method was used in the toxicity tests and for the additional studies. Current practice in environmental engineering relies on volatile suspended solids (VSS) as a measure of active biomass in activated sludge. After an improved ATP procedure was developed, ATP was investigated for estimation of active biomass. The fate of DCP in the toxicity tests was studied and an adsorptive mechanism was proposed that was based on membrane solubility. This mechanism explained the fate of DCP in the toxicity tests and is useful for understanding the fate of DCP in activated sludge.

  19. Screening antifungal activities of selected medicinal plants.

    PubMed

    Quiroga, E N; Sampietro, A R; Vattuone, M A

    2001-01-01

    Plants synthesise a vast array of secondary metabolites that are gaining importance for their biotechnological applications. The antifungal activity of the ethanolic extracts of ten Argentinean plants used in native medicine is reported. Antifungal assays included radial growth inhibition, disk and well diffusion assays and growth inhibition by broth dilution tests. The chosen test fungi were yeasts, microfungi and wood-rot causing Basidiomycetes. Extracts of Larrea divaricata, Zuccagnia punctata and Larrea cuneifolia displayed remarkable activity in the assays against the majority of the test fungi. In addition to the former plants, Prosopanche americana also inhibited yeast growth. PMID:11137353

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

    SciTech Connect

    Frank, C.W.; Anderson, T.D.; Cooley, C.R.; Hain, K.E.; Lien, S.C.T. . Office of Technology Development); Snipes, R.L. ); Erickson, M.D. )

    1991-01-01

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

  1. Effectiveness of timed and non-timed second appointments in improving uptake in breast cancer screening

    PubMed Central

    Hudson, Sue; Brazil, Debbie; Teh, William; Duffy, Stephen W

    2016-01-01

    Objectives To estimate the effect on breast screening uptake of delayed, targeted, second timed appointments in women who did not take up an initial breast cancer screening appointment offer. Methods Non-attending women received a four-month delayed second timed appointment following non-response to the initial invitation and the normal open invitation sent to non-attenders. A comparison group was sent a four-month delayed additional open invitation. Results Response to the second timed appointments (percentage of re-invited women eventually attending in this episode) was 20%, corresponding to an estimated increase on total uptake of 6%. Response was highest in women who had previously attended screens. Response in the women offered an additional delayed open invitation was 7.5%, corresponding to an estimated 2.3% increase in overall uptake. Conclusions Second timed appointments were almost three times as effective as additional open invitation. They should be targeted at women most likely to attend. A randomized study of second timed appointments versus open invitations should be conducted. PMID:26940961

  2. Social–Cognitive Predictors of Low-Income Parents’ Restriction of Screen Time Among Preschool-Aged Children

    PubMed Central

    Lampard, Amy M.; Jurkowski, Janine M.; Davison, Kirsten K.

    2015-01-01

    Parents’ rules regarding child television, DVD, video game, and computer use (screen time) have been associated with lower screen use in children. This study aimed to identify modifiable correlates of this behavior by examining social–cognitive predictors of parents’ restriction of child screen time. Low-income parents (N = 147) of preschool-aged children (2–6 years) completed self-administered questionnaires examining parent and child screen time, parent restriction of screen time, self-efficacy to restrict screen time, and beliefs about screen time. Structural equation modeling results indicated that greater self-efficacy to restrict screen time (β = .29, p = .016) and greater perceived importance of restricting child screen use (β = .55, p < .001) were associated with greater restriction of child screen use, after controlling for parent screen time. Family-based interventions that consider broader attitudinal factors around child screen time may be necessary to engage parents in restricting screen use. PMID:23239766

  3. Screening for Chlamydial Cervicitis in a Sexually Active University Population.

    ERIC Educational Resources Information Center

    Malotte, C. Kevin; And Others

    1990-01-01

    Enzyme-linked immunoabsorbent assays to detect chlamydial cervicitis were performed on samples from 1,320 sexually active university women. Seventy-five had positive tests. Demographic, history, symptom, and physical examination variables were insufficient to predict infection accurately. Concludes that screening during routine visits with this…

  4. A Drosophila Genome-Wide Screen Identifies Regulators of Steroid Hormone Production and Developmental Timing.

    PubMed

    Danielsen, E Thomas; Moeller, Morten E; Yamanaka, Naoki; Ou, Qiuxiang; Laursen, Janne M; Soenderholm, Caecilie; Zhuo, Ran; Phelps, Brian; Tang, Kevin; Zeng, Jie; Kondo, Shu; Nielsen, Christian H; Harvald, Eva B; Faergeman, Nils J; Haley, Macy J; O'Connor, Kyle A; King-Jones, Kirst; O'Connor, Michael B; Rewitz, Kim F

    2016-06-20

    Steroid hormones control important developmental processes and are linked to many diseases. To systematically identify genes and pathways required for steroid production, we performed a Drosophila genome-wide in vivo RNAi screen and identified 1,906 genes with potential roles in steroidogenesis and developmental timing. Here, we use our screen as a resource to identify mechanisms regulating intracellular levels of cholesterol, a substrate for steroidogenesis. We identify a conserved fatty acid elongase that underlies a mechanism that adjusts cholesterol trafficking and steroidogenesis with nutrition and developmental programs. In addition, we demonstrate the existence of an autophagosomal cholesterol mobilization mechanism and show that activation of this system rescues Niemann-Pick type C1 deficiency that causes a disorder characterized by cholesterol accumulation. These cholesterol-trafficking mechanisms are regulated by TOR and feedback signaling that couples steroidogenesis with growth and ensures proper maturation timing. These results reveal genes regulating steroidogenesis during development that likely modulate disease mechanisms. PMID:27326933

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

    PubMed

    Tuntland, Micheal L; Fung, L W-M

    2016-10-01

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

  6. Time activities at the BIPM

    NASA Technical Reports Server (NTRS)

    Thomas, Claudine

    1995-01-01

    The generation and dissemination of International Atomic Time, TAI, and of Coordinated Universal Time, UTC, are explicitly mentioned in the list of the principal tasks of the BIPM, recalled in the Comptes Rendus of the 18th Conference Generale des Poids et Mesures, in 1987. These tasks are fulfilled by the BIPM Time Section, thanks to international cooperation with national timing centers, which maintain, under metrological conditions, the clocks used to generate TAI. Besides the current work of data collection and processing, research activities are carried out in order to adapt the computation of TAI to the most recent improvements occurring in the time and frequency domains. Studies concerning the application of general relativity and pulsar timing to time metrology are also actively pursued. This paper summarizes the work done in all these fields and outlines future projects.

  7. Antituberculosis Activity of the Molecular Libraries Screening Center Network Library

    PubMed Central

    MADDRY, JOSEPH A.; ANANTHAN, SUBRAMANIAM; GOLDMAN, ROBERT C.; HOBRATH, JUDITH V.; KWONG, CECIL D.; MADDOX, CLINTON; RASMUSSEN, LYNN; REYNOLDS, ROBERT C.; SECRIST, JOHN A.; SOSA, MELINDA I.; WHITE, E. LUCILE; ZHANG, WEI

    2009-01-01

    SUMMARY There is an urgent need for the discovery and development of new antitubercular agents that target novel biochemical pathways and treat drug-resistant forms of the disease. One approach to addressing this need is through high-throughput screening of drug-like small molecule libraries against the whole bacterium in order to identify a variety of new, active scaffolds that will stimulate additional biological research and drug discovery. Through the Molecular Libraries Screening Center Network, the NIAID Tuberculosis Antimicrobial Acquisition and Coordinating Facility tested a 215,110-compound library against M. tuberculosis strain H37Rv. A medicinal chemistry survey of the results from the screening campaign is reported herein. PMID:19783214

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

    NASA Astrophysics Data System (ADS)

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

    2011-06-01

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

  9. Screen time and sleep among school-aged children and adolescents: a systematic literature review.

    PubMed

    Hale, Lauren; Guan, Stanford

    2015-06-01

    We systematically examined and updated the scientific literature on the association between screen time (e.g., television, computers, video games, and mobile devices) and sleep outcomes among school-aged children and adolescents. We reviewed 67 studies published from 1999 to early 2014. We found that screen time is adversely associated with sleep outcomes (primarily shortened duration and delayed timing) in 90% of studies. Some of the results varied by type of screen exposure, age of participant, gender, and day of the week. While the evidence regarding the association between screen time and sleep is consistent, we discuss limitations of the current studies: 1) causal association not confirmed; 2) measurement error (of both screen time exposure and sleep measures); 3) limited data on simultaneous use of multiple screens, characteristics and content of screens used. Youth should be advised to limit or reduce screen time exposure, especially before or during bedtime hours to minimize any harmful effects of screen time on sleep and well-being. Future research should better account for the methodological limitations of the extant studies, and seek to better understand the magnitude and mechanisms of the association. These steps will help the development and implementation of policies or interventions related to screen time among youth. PMID:25193149

  10. Screen Time and Sleep among School-Aged Children and Adolescents: A Systematic Literature Review

    PubMed Central

    Hale, Lauren; Guan, Stanford

    2015-01-01

    Summary We systematically examined and updated the scientific literature on the association between screen time (e.g., television, computers, video games, and mobile devices) and sleep outcomes among school-aged children and adolescents. We reviewed 67 studies published from 1999 to early 2014. We found that screen time is adversely associated with sleep outcomes (primarily shortened duration and delayed timing) in 90% of studies. Some of the results varied by type of screen exposure, age of participant, gender, and day of the week. While the evidence regarding the association between screen time and sleep is consistent, we discuss limitations of the current studies: 1.) causal association not confirmed; 2.) measurement error (of both screen time exposure and sleep measures); 3.) limited data on simultaneous use of multiple screens, characteristics and content of screens used. Youth should be advised to limit or reduce screen time exposure, especially before or during bedtime hours to minimize any harmful effects of screen time on sleep and well-being. Future research should better account for the methodological limitations of the extant studies, and seek to better understand the magnitude and mechanisms of the association. These steps will help the development and implementation of policies or interventions related to screen time among youth. PMID:25193149

  11. Screening for lipase activity in the oil palm.

    PubMed

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

    2000-12-01

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

  12. Application of Protein Expression Profiling to Screen Chemicals for Androgenic Activity.

    EPA Science Inventory

    Protein expression changes can be used for detection of biomarkers that can be applied diagnostically to screen chemicals for endocrine modifying activity. In this study, Surface Enhanced Laser Desorption/Ionization Time-of-Flight Mass Spectrometry (SELDI-TOF-MS) coupled with a s...

  13. The Family Context of Low-Income Parents Who Restrict Child Screen Time

    PubMed Central

    Jurkowski, Janine M.; Davison, Kirsten K.

    2013-01-01

    Abstract Background The American Academy of Pediatrics recommends that parents restrict child screen time to two hours per day, but many preschool-aged children exceed this viewing recommendation. Modifying children's viewing habits will require collaborating with parents, but little is known about the factors that influence parents' capacity for effective screen-related parenting. This study aimed to identify the demographic, family and community contextual factors associated with low-income parents' restriction of child screen time. Methods Parents (N=146) of children (age 2–5 years) attending Head Start centers in the United States completed a self-report survey in 2010 assessing parent and child screen use (television, DVD, video, video games, and leisure-time computer use), parent restriction of child screen time, and family (parent stress, social support, and life pressures) and community (neighborhood safety and social capital) factors. Results Children were more likely to meet the American Academy of Pediatrics screen time recommendation if their parent reported high restriction of child screen time. Parent and child demographic characteristics were not associated with parents' restriction of child screen time. In multivariate analysis, less parent screen time, fewer parent life pressures, and greater social support were associated with parents' high restriction of screen time. Conclusion Family contextual factors may play an important role in enabling low-income parents to restrict their children's screen time. When counseling low-income parents about the importance of restricting child screen time, practitioners should be sensitive to family contextual factors that may influence parents' capacity to implement this behavior change. PMID:24004326

  14. Screen time is associated with dietary intake in overweight Canadian children☆☆☆★★★

    PubMed Central

    Shang, Lei; Wang, JiaWei; O'Loughlin, Jennifer; Tremblay, Angelo; Mathieu, Marie-Ève; Henderson, Mélanie; Gray-Donald, Katherine

    2015-01-01

    Objectives To describe the relationship between screen time and dietary intake among children, and to examine this association in relation to body weight. Methods A cross-sectional analysis of 630 Canadian children aged 8–10 years with at least one obese biological parent. Measurements included body mass index (BMI), screen time (television, video game, computer), physical activity (accelerometer over 7 days), and diet (three 24-hour recalls for the calculation of the Canadian Healthy Eating Index (HEI-C)). Multivariate linear regression models were used to describe the relationship between screen time (≥ 2 h/d vs. < 2 h/d) and intake of nutrients and foods among healthy weight and overweight/obese children. Results The overall median [interquartile range] daily screen time was 2.2 [2.4] hours and 43% of children had a BMI of ≥ 85th percentile. Longer screen time above the recommendation (≥ 2 h/d) was associated with higher intake of energy (74 kcal, SE = 35), lower intake of fiber (− 0.6 g/1000 kcal, SE = 0.2) and vegetables & fruit (− 0.3 serving/1000 kcal, SE = 0.1) among all participants and with higher estimates in the overweight subgroup. An overall lower HEI-C (− 1.6, SE = 0.8) was also observed among children with screen time of ≥ 2 h/d. Among children of < 85th BMI percentile, longer screen time was associated with lower intake of vegetables & fruit (− 0.3 serving/1000 kcal, SE = 0.1) only. Conclusion Screen time is associated with less desirable food choices, particularly in overweight children. PMID:26844082

  15. The New Screen Time: Computers, Tablets, and Smartphones Enter the Equation

    ERIC Educational Resources Information Center

    Wiles, Bradford B.; Schachtner, Laura; Pentz, Julie L.

    2016-01-01

    Emerging technologies attract children and push parents' and caregivers' abilities to attend to their families. This article presents recommendations related to the new version of screen time, which includes time with computers, tablets, and smartphones. Recommendations are provided for screen time for very young children and those in middle and…

  16. Physical activity and screen-media-related parenting practices have different associations with children's objectively measured physical activity

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Children's physical activity (PA) is inversely associated with children's weight status. Parents may be an important influence on children's PA by restricting sedentary time or supporting PA. The aim of this study was to investigate the association of PA and screen-media–related [television (TV) and...

  17. INDUSTRIAL/MILITARY ACTIVITY-INITIATED ACCIDENT SCREENING ANALYSIS

    SciTech Connect

    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.

  18. Screening of Tanzanian medicinal plants for anti-Candida activity

    PubMed Central

    Runyoro, Deborah KB; Matee, Mecky IN; Ngassapa, Olipa D; Joseph, Cosam C; Mbwambo, Zakaria H

    2006-01-01

    Background Candida albicans has become resistant to the already limited, toxic and expensive anti-Candida agents available in the market. These factors necessitate the search for new anti-fungal agents. Methods Sixty-three plant extracts, from 56 Tanzanian plant species obtained through the literature and interviews with traditional healers, were evaluated for anti-Candida activity. Aqueous methanolic extracts were screened for anti-Candida activity by bioautography agar overlay method, using a standard strain of Candida albicans (ATCC 90028). Results Twenty- seven (48%) out of the 56 plants were found to be active. Extracts of the root barks of Albizia anthelmintica and Balanites aegyptiaca, and roots of Plectranthus barbatus showed strong activity. Conclusion The extracts that showed strong anti-Candida activity are worth of further investigation in order to isolate and identify the active compounds. PMID:16571139

  19. Cytotoxic activity screening of some indigenous Thai plants.

    PubMed

    Prayong, P; Barusrux, S; Weerapreeyakul, N

    2008-12-01

    The 50% ethanolic extracts from 14 plant species used in Thai traditional folklore were screened for cytotoxic activity against a malignant human hepatoma (HepG2) cell line and a normal African green monkey kidney (Vero) cell line. The extracts of Polyalthia evecta and Erythroxylum cuneatum showed potent anticancer activity in the HepG2 cell line with IC(50) of 70+/-3 microg/ml and 64+/-4 microg/ml, respectively. P. evecta demonstrated more selectivity to the HepG2 than the Vero cell (selectivity index>14.3) indicating its potential for biopharmaceutical use. PMID:18664377

  20. Beyond screening: tailoring physical activity options with the EASY tool.

    PubMed

    Chodzko-Zajko, Wojtek J; Resnick, Barbara; Ory, Marcia G

    2012-06-01

    The development and dissemination of the EASY tool provides a resource to facilitate access to information about physical activity for older adults, particularly with regard to specific physical activity recommendations for individuals with chronic medical conditions. Health care providers and older adults can use the EASY tool to provide a flexible, tailored approach to screening. This approach will better inform both older adults and their health care providers about safe physical activity programs with appropriate injury management strategies. The identification of a broad range of activities appropriate for different health circumstances and situations will enable a greater number of older adults to engage in physical activity/exercises that will improve their health and functioning. PMID:24073117

  1. Bioluminescent, Nonlytic, Real-Time Cell Viability Assay and Use in Inhibitor Screening

    PubMed Central

    Zhou, Wenhui; Meisenheimer, Poncho; Vidugiris, Gediminas; Cali, James J.; Gautam, Prson; Wennerberg, Krister; Vidugiriene, Jolanta

    2015-01-01

    Abstract Real-time continuous monitoring of cellular processes offers distinct advantages over traditional endpoint assays. A comprehensive representation of the changes occurring in live cells over the entire length of an experiment provides information about the biological status of the cell and informs decisions about the timing of treatments or the use of other functional endpoint assays. We describe a homogeneous, nonlytic, bioluminescent assay that measures cell viability in real time. This time-dependent measurement allowed us to monitor cell health for 72 h from the same test samples, distinguish differential cell growth, and investigate drug mechanism of action by analyzing time- and dose-dependent drug effects. The real-time measurements also allowed us to detect cell death immediately (>75% signal decrease within 15 min of digitonin addition), analyze drug potency versus efficacy, and identify cytostatic versus toxic drug effects. We screened an oncology compound library (Z′ = 0.7) and identified compounds with varying activity at different time points (1.6% of the library showed activity within 3 h, whereas 35.4% showed a response by 47 h). The assay compared well with orthogonal endpoint cell viability assays and additionally provided data at multiple time points and the opportunity to multiplex assays on the same cells. To test the advantage of time-dependent measurements to direct optimal timing of downstream applications, we used the real-time cell viability assay to determine the ideal time to measure caspase activity by monitoring the onset of cell death and multiplexing a luminescent caspase activation assay on the same test samples. PMID:26383544

  2. Drug Discovery for Duchenne Muscular Dystrophy via Utrophin Promoter Activation Screening

    PubMed Central

    Moorwood, Catherine; Lozynska, Olga; Suri, Neha; Napper, Andrew D.; Diamond, Scott L.; Khurana, Tejvir S.

    2011-01-01

    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. PMID:22028826

  3. The roles of general and technology-related parenting in managing youth screen time.

    PubMed

    Sanders, Wesley; Parent, Justin; Forehand, Rex; Breslend, Nicole Lafko

    2016-08-01

    This study examines the associations of 2 types of parenting practices-general adaptive parenting and technology-related strategies-with youth screen time. We hypothesized that technology-related parenting focused on behavioral control would relate directly to screen time and serve to link general parenting to screen time. Participants were 615 parents drawn from 3 community samples of families with children across 3 development stages: young childhood (3-7 years; n = 210), middle childhood (8-12 years; n = 200), and adolescents (13-17 years; n = 205). Using structural equation modeling, we found that general adaptive parenting was not related to child screen time but was positively related to technology-related parenting strategies for all 3 samples. For the young and, to some extent, middle childhood samples, but not for the adolescent sample, general adaptive parenting was positively linked to youth screen time through technology-related parenting strategies. (PsycINFO Database Record PMID:26751759

  4. Neighbourhood urban form and individual-level correlates of leisure-based screen time in Canadian adults

    PubMed Central

    McCormack, Gavin R; Mardinger, Cynthia

    2015-01-01

    Objectives Despite evidence for an association between the built environment and physical activity, less evidence exists regarding relations between the built environment and sedentary behaviour. This study investigated the extent to which objectively assessed and self-reported neighbourhood walkability, in addition to individual-level characteristics, were associated with leisure-based screen time in adults. We hypothesised that leisure-based screen time would be lower among adults residing in objectively assessed and self-reported ‘high walkable’ versus ‘low walkable’ neighbourhoods. Setting The study was undertaken in Calgary, Alberta, Canada in 2007/2008. Participants A random cross-section of adults who provided complete telephone interview and postal survey data (n=1906) was included. Captured information included leisure-based screen time, moderate-intensity and vigorous-intensity physical activity, perceived neighbourhood walkability, sociodemographic characteristics, self-reported health status, and self-reported height and weight. Based on objectively assessed built characteristics, participant's neighbourhoods were identified as being low, medium or high walkable. Primary and secondary outcome measures Using multiple linear regression, hours of leisure-based screen time per day was regressed on self-reported and objectively assessed walkability adjusting for sociodemographic and health-related covariates. Results Compared to others, residing in an objectively assessed high walkable neighbourhood, women, having a college education, at least one child at home, a household income ≥$120 000/year, and a registered motor vehicle at home, reporting very good-to-excellent health and healthy weight, and achieving 60 min/week of vigorous-intensity physical activity were associated (p<0.05) with less leisure-based screen time. Marital status, dog ownership, season, self-reported walkability and achieving 210 min of moderate-intensity physical

  5. Neighborhood disorder and screen time among 10-16 year old Canadian youth: A cross-sectional study

    PubMed Central

    2012-01-01

    Background Screen time activities (e.g., television, computers, video games) have been linked to several negative health outcomes among young people. In order to develop evidence-based interventions to reduce screen time, the factors that influence the behavior need to be better understood. High neighborhood disorder, which may encourage young people to stay indoors where screen time activities are readily available, is one potential factor to consider. Methods Results are based on 15,917 youth in grades 6-10 (aged 10-16 years old) who participated in the Canadian 2009/10 Health Behaviour in School-aged Children Survey (HBSC). Total hours per week of television, video games, and computer use were reported by the participating students in the HBSC student questionnaire. Ten items of neighborhood disorder including safety, neighbors taking advantage, drugs/drinking in public, ethnic tensions, gangs, crime, conditions of buildings/grounds, abandoned buildings, litter, and graffiti were measured using the HBSC student questionnaire, the HBSC administrator questionnaire, and Geographic Information Systems. Based upon these 10 items, social and physical neighborhood disorder variables were derived using principal component analysis. Multivariate multilevel logistic regression analyses were used to examine the relationship between social and physical neighborhood disorder and individual screen time variables. Results High (top quartile) social neighborhood disorder was associated with approximately 35-45% increased risk of high (top quartile) television, computer, and video game use. Physical neighborhood disorder was not associated with screen time activities after adjusting for social neighborhood disorder. However, high social and physical neighborhood disorder combined was associated with approximately 40-60% increased likelihood of high television, computer, and video game use. Conclusion High neighborhood disorder is one environmental factor that may be important

  6. Screen Time at Home and School among Low-Income Children Attending Head Start

    PubMed Central

    Fletcher, Erica N.; Whitaker, Robert C.; Marino, Alexis J.; Anderson, Sarah E.

    2013-01-01

    Objective To describe the patterns of screen viewing at home and school among low-income preschool-aged children attending Head Start and identify factors associated with high home screen time in this population. Few studies have examined both home and classroom screen time, or included computer use as a component of screen viewing. Methods Participants were 2221 low-income preschool-aged children in the United States studied in the Head Start Family and Child Experiences Survey (FACES) in spring 2007. For 5 categories of screen viewing (television, video/DVD, video games, computer games, other computer use), we assessed children’s typical weekday home (parent-reported) and classroom (teacher-reported) screen viewing in relation to having a television in the child’s bedroom and sociodemographic factors. Results Over half of children (55.7%) had a television in their bedroom, and 12.5% had high home screen time (>4 hours/weekday). Television was the most common category of home screen time, but 56.6% of children had access to a computer at home and 37.5% had used it on the last typical weekday. After adjusting for sociodemographic characteristics, children with a television in their bedroom were more likely to have high home screen time [odds ratio=2.57 (95% confidence interval: 1.80–3.68)]. Classroom screen time consisted almost entirely of computer use; 49.4% of children used a classroom computer for ≥1 hour/week, and 14.2% played computer games at school ≥5 hours/week. Conclusions In 2007, one in eight low-income children attending Head Start had >4 hours/weekday of home screen time, which was associated with having a television in the bedroom. In the Head Start classroom, television and video viewing were uncommon but computer use was common. PMID:24891924

  7. What Works -- and Doesn't -- to Manage Your Tot's Screen Time

    MedlinePlus

    ... And Doesn't -- to Manage Your Tot's Screen Time Key points: setting regular schedules for media use, ... learning and entertainment, but what works when it's time to sign off? A new study into the ...

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

    PubMed Central

    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. PMID:25593396

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

    PubMed

    Streb, Judith; Kammer, Thomas; Spitzer, Manfred; Hille, Katrin

    2015-01-01

    This paper reports accelerometer and electronic dairy data on typical daily activities of 139 school students from grade six and nine. Recordings covered a typical school day for each student and lasted on average for 23 h. Screen activities (watching television and using the computer) are compared to several other activities performed while sitting (e.g., playing, eating, sitting in school, and doing homework). Body movement was continuously recorded by four accelerometers and transformed into a motion sore. Our results show that extremely low motion scores, as if subjects were freezing, emerge to a greater extent in front of screens compared to other investigated activities. Given the substantial amount of time young people spend in front of screens and the rising obesity epidemic, our data suggest a mechanism for the association of screen time and obesity. PMID:25955531

  10. Extremely Reduced Motion in Front of Screens: Investigating Real-World Physical Activity of Adolescents by Accelerometry and Electronic Diary

    PubMed Central

    Streb, Judith; Kammer, Thomas; Spitzer, Manfred; Hille, Katrin

    2015-01-01

    This paper reports accelerometer and electronic dairy data on typical daily activities of 139 school students from grade six and nine. Recordings covered a typical school day for each student and lasted on average for 23 h. Screen activities (watching television and using the computer) are compared to several other activities performed while sitting (e.g., playing, eating, sitting in school, and doing homework). Body movement was continuously recorded by four accelerometers and transformed into a motion sore. Our results show that extremely low motion scores, as if subjects were freezing, emerge to a greater extent in front of screens compared to other investigated activities. Given the substantial amount of time young people spend in front of screens and the rising obesity epidemic, our data suggest a mechanism for the association of screen time and obesity. PMID:25955531

  11. Increased Screen Time: Implications for Early Childhood Development and Behavior.

    PubMed

    Radesky, Jenny S; Christakis, Dimitri A

    2016-10-01

    The authors review trends in adoption of new digital technologies (eg, mobile and interactive media) by families with young children (ages 0-8 years), continued use of television and video games, and the evidence for learning from digital versus hands-on play. The authors also discuss continued concerns about health and developmental/behavioral risks of excessive media use for child cognitive, language, literacy, and social-emotional development. This evidence is then applied to clinical care in terms of the screening questions providers can use, tools available to providers and parents, and changes in anticipatory guidance. PMID:27565361

  12. Energy intake and expenditure during sedentary screen time and motion-controlled video gaming123

    PubMed Central

    Tate, Deborah F; Ward, Dianne S; Wang, Xiaoshan

    2012-01-01

    Background: Television watching and playing of video games (VGs) are associated with higher energy intakes. Motion-controlled video games (MC) may be a healthier alternative to sedentary screen-based activities because of higher energy expenditures, but little is known about the effects of these games on energy intakes. Objective: Energy intake, expenditure, and surplus (intake − expenditure) were compared during sedentary (television and VG) and active (MC) screen-time use. Design: Young adults (n = 120; 60 women) were randomly assigned to the following 3 groups: television watching, playing traditional VGs, or playing MCs for 1 h while snacks and beverages were provided. Energy intakes, energy expenditures, and appetites were measured. Results: Intakes across these 3 groups showed a trend toward a significant difference (P = 0.065). The energy expenditure (P < 0.001) was higher, and the energy surplus (P = 0.038) was lower, in MC than in television or VG groups. All conditions produced a mean (±SD) energy surplus as follows: 638 ± 408 kcal in television, 655 ± 533 kcal in VG, and 376 ± 487 kcal in MC groups. The OR for consuming ≥500 kcal in the television compared with the MC group was 3.2 (95% CI: 1.2, 8.4). Secondary analyses, in which the 2 sedentary conditions were collapsed, showed an intake that was 178 kcal (95% CI: 8, 349 kcal) lower in the MC condition than in the sedentary groups (television and VG). Conclusion: MCs may be a healthier alternative to sedentary screen time because of a lower energy surplus, but the playing of these games still resulted in a positive energy balance. This trial was registered at clinicaltrials.gov as NCT01523795. PMID:22760571

  13. Screening of some Nigerian plants for molluscicidal activity.

    PubMed

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

    1989-01-01

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

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

    PubMed Central

    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. PMID:26658480

  15. Reducing Youth Screen Time: Qualitative Metasynthesis of Findings on Barriers and Facilitators

    PubMed Central

    Minges, Karl E.; Salmon, Jo; Dunstan, David W.; Owen, Neville; Chao, Ariana; Whittemore, Robin

    2015-01-01

    Objective An integrated perspective on the relevant qualitative findings on the experience of screen time in youth can inform the development of hypotheses to be tested in future research and can guide the development of interventions to decrease sedentary behavior. The purpose of this qualitative metasynthesis was to explore parent, youth, and educational professionals’ perceptions of barriers to, and facilitators of, reducing youth screen time. Method Qualitative metasynthesis techniques were used to analyze and synthesize 15 qualitative studies of screen time among youth (11–18 years) meeting inclusion criteria. The phrases, quotes, and/or author interpretations (i.e., theme or subtheme) were recorded in a data display matrix to facilitate article comparisons. Codes were collapsed into 23 categories of similar conceptual meaning and 3 overarching themes were derived using thematic analysis procedures. Results Study sample sizes ranged from 6 to 270 participants from 6 countries. Data collection methods included focus groups (n = 6), interviews (n = 4), focus group and interviews (n = 4), and naturalistic observation (n = 1) with youth and/or parents. Data analysis techniques included thematic analysis (n = 9), content analysis (n = 3), grounded theory (n = 1), observation (n = 1), and interpretive phenomenological analysis (n = 1). Three thematic categories were identified: (a) youth’s norms—screen time is an integral part of daily life, and facilitates opportunities for entertainment, social interaction, and escapism; (b) family dynamics and parental roles—parents are conflicted and send mixed messages about the appropriate uses and amounts of screen time; and, (c) resources and environment—engagement in screen time is dependent on school, community, neighborhood, and home environmental contexts. Conclusions Screen time is an established norm in many youth cultures, presenting barriers to behavior change. Parents recognize the importance of reducing

  16. Screening of basidiomycetes in submerged cultivation based on antioxidant activity.

    PubMed

    Umeo, S H; Souza, G P N; Rapachi, P M; Garcia, D M; Paccola-Meirelles, L D; Valle, J S; Colauto, N B; Linde, G A

    2015-01-01

    Submerged cultivation of medicinal basidiomycetes is a reproducible and efficient method of producing mycelia and metabolites. The antioxidant activity indicates its medicinal properties and is an important tool for basidiomycete screening. In this study, we analyzed the production of mycelial biomass and exopolysaccharides and the antioxidant activity of basidiomycete strains in submerged cultivation. Twenty-five strains were used for submerged cultivation in extract malt medium, and the production of mycelial biomass and exopolysaccharides was evaluated. Antioxidant activity was determined using the 1,1-diphenyl-2-picrylhydrazyl method. Among the 25 evaluated strains, Lentinus crinitus produced the highest biomass, reaching 1190 ± 52 mg·L(-1)day(-1); Agaricus subrufescens strains had the highest exopolysaccharide production from 18.96 ± 0.15 to 20.97 ± 2.10 mg L(-1)·day(-1). Additionally, A. subrufescens showed the highest total antioxidant activity, reinforcing the therapeutic potential of this basidiomycete. No significant correlation was found between mycelial biomass or exopolysaccharide production and antioxidant activity; however, the results depended on each species and the strains of the same species. We found large variations in the production of mycelial biomass and exopolysaccharides and in antioxidant activity among different species and among strains of the same species. Thus, evaluating the total antioxidant activity is an important tool for identifying strains with biotechnological potential. PMID:26345925

  17. A TR-FRET-based functional assay for screening activators of CARM1.

    PubMed

    Zeng, Hao; Wu, Jiacai; Bedford, Mark T; Sbardella, Gianluca; Hoffmann, F Michael; Bi, Kun; Xu, Wei

    2013-05-10

    Epigenetics is an emerging field that demands selective cell-permeable chemical probes to perturb, especially in vivo, the activity of specific enzymes involved in modulating the epigenetic codes. Coactivator-associated arginine methyltransferase 1 (CARM1) is a coactivator of estrogen receptor α (ERα), the main target in human breast cancer. We previously showed that twofold overexpression of CARM1 in MCF7 breast cancer cells increased the expression of ERα-target genes involved in differentiation and reduced cell proliferation, thus leading to the hypothesis that activating CARM1 by chemical activators might be therapeutically effective in breast cancer. Selective, potent, cell-permeable CARM1 activators will be essential to test this hypothesis. Here we report the development of a cell-based, time-resolved (TR) FRET assay that uses poly(A) binding protein 1 (PABP1) methylation to monitor cellular activity of CARM1. The LanthaScreen TR-FRET assay uses MCF7 cells expressing GFP-PABP1 fusion protein through BacMam gene delivery system, methyl-PABP1 specific antibody, and terbium-labeled secondary antibody. This assay has been validated as reflecting the expression and/or activity of CARM1 and optimized for high throughput screening to identify CARM1 allosteric activators. This TR-FRET platform serves as a generic tool for functional screening of cell-permeable, chemical modulators of CARM1 for elucidation of its in vivo functions. PMID:23585185

  18. High-throughput screening assays for antibacterial and antifungal activities of Lactobacillus species.

    PubMed

    Inglin, Raffael C; Stevens, Marc J A; Meile, Lukas; Lacroix, Christophe; Meile, Leo

    2015-07-01

    We describe high-throughput screening techniques to rapidly detect either antimicrobial activity, using an agar-well diffusion assay in microtiter plates, or antifungal activity using an agar-spot assay in 24-well plates. 504 Lactobacillus isolates were screened with minimal laboratory equipment and screening rates of 2000-5000 individual antimicrobial interactions. PMID:25937247

  19. Screening of Thai medicinal plant extracts and their active constituents for in vitro antimalarial activity.

    PubMed

    Ichino, C; Soonthornchareonnon, N; Chuakul, W; Kiyohara, H; Ishiyama, A; Sekiguchi, H; Namatame, M; Otoguro, K; Omura, S; Yamada, H

    2006-04-01

    To discover antimalarial substances from plants cultivated in Thailand 80%-EtOH extracts from selected plants were screened for in vitro antimalarial activity against the drug resistant K1 strain of Plasmodium falciparum. In total, 86 Thai medicinal plant samples representing 48 species from 35 genera in 16 families were screened and two species (Polyalthia viridis and Goniothalamus marcanii) were found to show notable antimalarial activity (IC50: 10.0 and 6.3 microg/mL). Marcanine A and 16-hydroxycleroda-3,13(14)Z-dien-15,16-olide were identified as the respective major active constituents in P. viridis and G. marcanii, respectively. PMID:16557615

  20. A Microplate Format Assay for Real-Time Screening for New Aldolases that Accept Aryl-Substituted Acceptor Substrates.

    PubMed

    Ma, Huan; Enugala, Thilak Reddy; Widersten, Mikael

    2015-12-01

    Aldolases are potentially important biocatalysts for asymmetric synthesis of polyhydroxylated compounds. Fructose 6-phosphate aldolase (FSA) is of particular interest by virtue of its unusually relaxed dependency on phosphorylated substrates. FSA has been reported to be a promising catalyst of aldol addition involving aryl-substituted acceptors such as phenylacetaldehyde that can react with donor ketones such as hydroxyacetone. Improvement of the low intrinsic activity with bulky acceptor substrates of this type is of great interest but has been hampered by the lack of powerful screening protocols applicable in directed evolution strategies. Here we present a new screen allowing for direct spectrophotometric recording of retro-aldol cleavage. The assay utilizes an aldehyde reductase produced in vitro by directed evolution; it reduces the aldehyde product formed after cleavage of the aldol by FSA. The assay is suitable both for steady-state enzyme kinetics and for real-time activity screening in a 96-well format. PMID:26449620

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

    PubMed Central

    Roh, Changhyun; Jung, Uhee

    2012-01-01

    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. PMID:22408418

  2. Screening for enzyme activity in turbid suspensions with scattered light.

    PubMed

    Huber, Robert; Wulfhorst, Helene; Maksym, Lukas; Stehr, Regina; Pöhnlein, Martin; Jäger, Gernot; Spiess, Antje C; Büchs, Jochen

    2011-01-01

    New screening techniques for improved enzyme variants in turbid media are urgently required in many industries such as the detergent and food industry. Here, a new method is presented to measure enzyme activity in different types of substrate suspensions. This method allows a semiquantitative determination of protease activity using native protein substrates. Unlike conventional techniques for measurement of enzyme activity, the BioLector technology enables online monitoring of scattered light intensity and fluorescence signals during the continuous shaking of samples in microtiter plates. The BioLector technique is hereby used to monitor the hydrolysis of an insoluble protein substrate by measuring the decrease of scattered light. The kinetic parameters for the enzyme reaction (V(max,app) and K(m,app)) are determined from the scattered light curves. Moreover, the influence of pH on the protease activity is investigated. The optimal pH value for protease activity was determined to be between pH 8 to 11 and the activities of five subtilisin serine proteases with variations in the amino acid sequence were compared. The presented method enables proteases from genetically modified strains to be easily characterized and compared. Moreover, this method can be applied to other enzyme systems that catalyze various reactions such as cellulose decomposition. PMID:21302369

  3. Interactive vs passive screen time and nighttime sleep duration among school-aged children

    PubMed Central

    Yland, Jennifer; Guan, Stanford; Emanuele, Erin; Hale, Lauren

    2016-01-01

    Background Insufficient sleep among school-aged children is a growing concern, as numerous studies have shown that chronic short sleep duration increases the risk of poor academic performance and specific adverse health outcomes. We examined the association between weekday nighttime sleep duration and 3 types of screen exposure: television, computer use, and video gaming. Methods We used age 9 data from an ethnically diverse national birth cohort study, the Fragile Families and Child Wellbeing Study, to assess the association between screen time and sleep duration among 9-year-olds, using screen time data reported by both the child (n = 3269) and by the child's primary caregiver (n= 2770). Results Within the child-reported models, children who watched more than 2 hours of television per day had shorter sleep duration by approximately 11 minutes per night compared to those who watched less than 2 hours of television (β = −0.18; P < .001). Using the caregiver-reported models, both television and computer use were associated with reduced sleep duration. For both child- and parent-reported screen time measures, we did not find statistically significant differences in effect size across various types of screen time. Conclusions Screen time from televisions and computers is associated with reduced sleep duration among 9-year-olds, using 2 sources of estimates of screen time exposure (child and parent reports). No specific type or use of screen time resulted in significantly shorter sleep duration than another, suggesting that caution should be advised against excessive use of all screens. PMID:27540566

  4. Association between neighborhood socioeconomic status and screen time among pre-school children: a cross-sectional study

    PubMed Central

    2010-01-01

    Background Sedentary behavior is considered a separate construct from physical activity and engaging in sedentary behaviors results in health effects independent of physical activity levels. A major source of sedentary behavior in children is time spent viewing TV or movies, playing video games, and using computers. To date no study has examined the impact of neighborhood socioeconomic status (SES) on pre-school children's screen time behavior. Methods Proxy reports of weekday and weekend screen time (TV/movies, video games, and computer use) were completed by 1633 parents on their 4-5 year-old children in Edmonton, Alberta between November, 2005 and August, 2007. Postal codes were used to classified neighborhoods into low, medium or high SES. Multiple linear and logistic regression models were conducted to examine relationships between screen time and neighborhood SES. Results Girls living in low SES neighborhoods engaged in significantly more weekly overall screen time and TV/movie minutes compared to girls living in high SES neighborhoods. The same relationship was not observed in boys. Children living in low SES neighborhoods were significantly more likely to be video game users and less likely to be computer users compared to children living in high SES neighborhoods. Also, children living in medium SES neighborhoods were significantly less likely to be computer users compared to children living in high SES neighborhoods. Conclusions Some consideration should be given to providing alternative activity opportunities for children, especially girls who live in lower SES neighborhoods. Also, future research should continue to investigate the independent effects of neighborhood SES on screen time as well as the potential mediating variables for this relationship. PMID:20573262

  5. GPU-accelerated real-time IR smoke screen simulation and assessment of its obscuration

    NASA Astrophysics Data System (ADS)

    Wu, Xin; Zhang, Jian-qi; Huang, Xi; Liu, De-lian

    2012-01-01

    With the growing demand for the Battlefield Environment Simulation (BES), IR smoke screen, which is computationally expensive and absolutely indispensable, should be modeled true to life and correct in its thermal radiation characteristics. This paper analyzes the features of an IR smoke screen, and represents an IR smoke screen model based on light extinction, particle dispersion and temperature attenuation, which is calculated by GPU and rendered to screen in real time. Thus a method considering both the real-life in profile and the real-time in efficiency is presented. Additionally, the comparison between the simulated results and the measured data is made to verify the correctness of the smoke screen's obscuration, which illustrates the effect of its interference feature in an infrared scene.

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

    NASA Technical Reports Server (NTRS)

    Powers. W. Edward

    2010-01-01

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

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

    PubMed

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

    2016-01-01

    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. PMID:27010513

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

    NASA Astrophysics Data System (ADS)

    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.

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

    PubMed Central

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

    2016-01-01

    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. PMID:27010513

  10. Time to benefit for colorectal cancer screening: survival meta-analysis of flexible sigmoidoscopy trials

    PubMed Central

    Boscardin, W John; Stijacic-Cenzer, Irena; Lee, Sei J

    2015-01-01

    Objective To determine the time to benefit of using flexible sigmoidoscopy for colorectal cancer screening. Design Survival meta-analysis. Data sources A Cochrane Collaboration systematic review published in 2013, Medline, and Cochrane Library databases. Eligibility criteria Randomized controlled trials comparing screening flexible sigmoidoscopy with no screening. Trials with fewer than 100 flexible sigmoidoscopy screenings were excluded. Results Four studies were eligible (total n=459 814). They were similar for patients’ age (50-74 years), length of follow-up (11.2-11.9 years), and relative risk for colorectal cancer related mortality (0.69-0.78 with flexible sigmoidoscopy screening). For every 1000 people screened at five and 10 years, 0.3 and 1.2 colorectal cancer related deaths, respectively, were prevented. It took 4.3 years (95% confidence interval 2.8 to 5.8) to observe an absolute risk reduction of 0.0002 (one colorectal cancer related death prevented for every 5000 flexible sigmoidoscopy screenings). It took 9.4 years (7.6 to 11.3) to observe an absolute risk reduction of 0.001 (one colorectal cancer related death prevented for every 1000 flexible sigmoidoscopy screenings). Conclusion Our findings suggest that screening flexible sigmoidoscopy is most appropriate for older adults with a life expectancy greater than approximately 10 years. PMID:25881903

  11. More Screen Time, Less Face time – Implications for EHR Design

    PubMed Central

    Asan, Onur; Smith, Paul; Montague, Enid

    2014-01-01

    Rationale, aims and objectives Understanding the impact of health information technology on doctor-patient interaction is vital to designing better electronic health records (EHRs). This article quantitatively examines and compares clinically experienced physicians’ interactions with patients using paper or electronic health records in ambulatory primary care settings. Methods Clinical encounters using paper or electronic health records were recorded with high-resolution video cameras to capture physicians’ interactions with the health records and patients. All videos were coded using quantified video coding methodology to understand how physicians interacted with EHRs and patients through measuring eye gaze durations. Statistical analysis was conducted to compare the results of the paper and electronic health record visits. Results Eight experienced family medicine physicians and eighty patients participated in the study. A total of 80 visits, 40 with paper and 40 with EHRs were recorded. The proportion of time physicians spent gazing at medical records during EHR visits was significantly more than in paper chart visits (35.2% VS 22.1%, P=0.001). A significantly smaller proportion of physician time was spent gazing at the patient when using an EHR compared to when using a paper chart (52.6% VS 45.6%, P= 0.041). Shared gaze by both physician and patient at the records was not significantly different between the two settings. Conclusions For this group of family medicine physicians, more time was spent looking at the EHR screen than paper records and a little less time looking at the patient. These findings may negatively affect the patient perception of the visit with the physician and have implications for the design of future EHRs. PMID:24835678

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

    PubMed Central

    Geschwindner, Stefan; Carlsson, Johan F.; Knecht, Wolfgang

    2012-01-01

    The last two decades have seen remarkable progress and improvements in optical biosensor systems such that those are currently seen as an important and value-adding component of modern drug screening activities. In particular the introduction of microplate-based biosensor systems holds the promise to match the required throughput without compromising on data quality thus representing a sought-after complement to traditional fluidic systems. This article aims to highlight the application of the two most prominent optical biosensor technologies, namely surface plasmon resonance (SPR) and optical waveguide grating (OWG), in small-molecule screening and will present, review and discuss the advantages and disadvantages of different assay formats on these platforms. A particular focus will be on the specific advantages of the inhibition in solution assay (ISA) format in contrast to traditional direct binding assays (DBA). Furthermore we will discuss different application areas for both fluidic as well as plate-based biosensor systems by considering the individual strength of the platforms. PMID:22666031

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

    ERIC Educational Resources Information Center

    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.

  14. The effect of radiation screens on Nordic time series of mean temperature

    NASA Astrophysics Data System (ADS)

    Nordli, P. Ø.; Alexandersson, H.; Frich, P.; Førland, E. J.; Heino, R.; Jónsson, T.; Tuomenvirta, H.; Tveito, O. E.

    1997-12-01

    A short survey of the historical development of temperature radiation screens is given based upon research in the archives of the Nordic meteorological institutes. In the middle of the nineteenth century most thermometer stands were open shelters, free-standing or fastened to a window or wall. Most of these were soon replaced by wall or window screens, i.e. small wooden or metal cages. Large free-standing screens were also introduced in the nineteenth century, but it took to the 1980s before they had replaced the wall screens completely in all Nordic countries. During recent years, small cylindrical screens suitable for automatic weather stations have been introduced. At some stations they have replaced the ordinary free-standing screen as part of a gradual move towards automation.The first free-standing screens used in the Nordic countries were single louvred. They were later improved by double louvres. Compared with observations from ventilated thermometers the monthly mean temperatures in the single louvred screens were 0.2-0.4°C higher during May-August, whereas in the double louvred screens the temperatures were unbiased. Unless the series are adjusted, this improvement may lead to inhomogeneities in long climatic time series.The change from wall screen to free-standing screen also involved a relocation from the microclimatic influence of a house to a location free from obstacles. Tests to evaluate the effect of relocation by parallel measurements yielded variable results. However, the bulk of the tests showed no effect of the relocation in winter, whereas in summer the wall screen tended to be slightly warmer (0.0-0.3°C) than the double louvred screen. At two Norwegian sites situated on steep valley slopes, the wall screen was ca. 0.5°C colder in midwinter.The free-standing Swedish shelter, which was used at some stations up to 1960, seems to have been overheated in spring and summer (maximum overheating of about 0.4°C in early summer). The new screen for

  15. Associations among evening snacking, screen time, weight status, and overall diet quality in young adolescents.

    PubMed

    Ciccone, Jillian; Woodruff, Sarah J; Fryer, Katherine; Campbell, Ty; Cole, Mary

    2013-07-01

    The purpose of this study was to determine the associations among evening snacking (food choices, portion sizes), afterschool-evening screen time, overall diet quality, and weight status. Participants consisted of 1008 young adolescents (secondary analyses, n = 651) from schools in Windsor-Essex, Ontario. The Web-based Food Behaviour Questionnaire, including a 24-h diet recall, was used to assess eating and screen time behaviours (television and video and computer games), as well as nutrient intake; height and weight for BMI were measured using a stadiometer. Results indicated that the majority of participants (62%) consumed an evening snack that contributed approximately 11% of their daily caloric intake. Evening snacking was associated with an overall good diet quality compared with that of non-evening snackers (p < 0.001). Increased afterschool-evening screen time was associated with fewer evening snack servings of vegetables and fruit (p < 0.05) and an overall increase in evening snack food portion sizes (p < 0.001). After accounting for other evening snacking factors, participants with greater than 6 h of afterschool-evening screen time were less likely to have a good overall diet quality compared with those with less than 1 h of afterschool-evening screen time. Therefore, increased screen time, because it is associated with greater evening snack portion sizes and overall poor diet quality, is of great concern regarding young adolescents' evening behaviour. PMID:23980738

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

    PubMed

    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. PMID:15907878

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

    PubMed

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

    2016-07-19

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

  18. High-throughput screening of phosphodiesterase activity in living cells.

    PubMed

    Rich, Thomas C; Karpen, Jeffrey W

    2005-01-01

    Phosphodiesterases (PDEs) hydrolyze the second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine 5'-monophosphate (cGMP) and play a crucial role in the termination and spatial segregation of cyclic nucleotide signals. Despite a wealth of molecular information, very little is known about how PDEs regulate cAMP and cGMP signals in living cells because conventional methods lack the necessary spatial and temporal resolution. We present here a sensitive optical method for monitoring cAMP levels and PDE activity near the membrane, using cyclic nucleotide-gated (CNG) ion channels as sensors. These channels are directly opened by the binding of cyclic nucleotides and allow cations to cross the membrane. The olfactory channel A subunit (CNGA2) has been genetically modified to improve its cAMP sensitivity and specificity. Channel activity is assessed by measuring Ca2+ influx using standard fluorometric techniques. In addition to studying PDEs in their native setting, the approach should be particularly useful in high-throughput screening assays to test for compounds that affect PDE activity, as well as the activities of the many G protein-coupled receptors that cause changes in intracellular cAMP. PMID:15988054

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

    PubMed Central

    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.

    2016-01-01

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

  20. Benefits of Time Correlation Measurements for Passive Screening

    NASA Astrophysics Data System (ADS)

    Murer, David; Blackie, Douglas; Peerani, Paolo

    2014-02-01

    The “FLASH Portals Project” is a collaboration between Arktis Radiation Detectors Ltd (CH), the Atomic Weapons Establishment (UK), and the Joint Research Centre (European Commission), supported by the Technical Support Working Group (TSWG). The program's goal was to develop and demonstrate a technology to detect shielded special nuclear materials (SNM) more efficiently and less ambiguously by exploiting time correlation. This study presents experimental results of a two-sided portal monitor equipped with in total 16 4He fast neutron detectors as well as four polyvinyltoluene (PVT) plastic scintillators. All detectors have been synchronized to nanosecond precision, thereby allowing the resolution of time correlations from timescales of tens of microseconds (such as (n, γ) reactions) down to prompt fission correlations directly. Our results demonstrate that such correlations can be detected in a typical radiation portal monitor (RPM) geometry and within operationally acceptable time scales, and that exploiting these signatures significantly improves the performance of the RPM compared to neutron counting. Furthermore, the results show that some time structure remains even in the presence of heavy shielding, thus significantly improving the sensitivity of the detection system to shielded SNM.

  1. Busy lifestyles and mammography screening: time pressure and women's reattendance likelihood.

    PubMed

    Brown, Stephen L; Gibney, Triecia M; Tarling, Rachel

    2013-01-01

    Time pressure is often cited as a reason for non-attendance at mammography screening, although evidence from other areas of psychology suggests that time pressure can improve performance when barriers such as time pressure provide a challenge. We predicted that time pressure would negatively predict attendance in women whose self-efficacy for overcoming time pressure is low, but positively predict attendance when self-efficacy is high. Time pressure was operationalised as the self-reported number of dependent children and others, and average number of working hours per week. Australian women were surveyed after being invited to attend second or subsequent screenings at a free public screening service, and subsequent attendance monitored until six months after screening was due. The majority (87.5%) attended screening. Women with more dependent children and higher self-efficacy showed greater attendance likelihood, and women with fewer non-child dependants and lower self-efficacy were less likely to attend. Working hours did not predict attendance. Findings provide partial support for the idea that time pressure acts as a challenge for women with high self-efficacy. PMID:23397934

  2. [Progresses in screening active compounds from herbal medicine by affinity chromatography].

    PubMed

    Feng, Ying-shu; Tong, Shan-shan; Xu, Xi-ming; Yu, Jiang-nan

    2015-03-01

    Affinity chromatography is a chromatographic method for separating molecules using the binding characteristics of the stationary phase with potential drug molecules. This method can be performed as a high throughput screening method and a chromatographic separation method to screen a variety of active drugs. This paper summarizes the history of affinity chromatography, screening technology of affinity chromatography, and application of affinity chromatography in screening bio-active compounds in herbal medicines, and then discusses its application prospects, in order to broaden applications of the affinity chromatography in drug screening. PMID:26226740

  3. Factors associated with screen time among school-age children in Korea.

    PubMed

    Ham, Ok Kyung; Sung, Kyung Mi; Kim, Hee Kyung

    2013-12-01

    The purpose of this study was to investigate the association of sociodemographic, psychosocial, and behavioral characteristics with screen time among school-age children in Korea. This study employed a nonexperimental, cross-sectional study design. A total of 370 children attending four elementary schools participated in the study. Self-report method was used, and instruments included screen time (time spent on TV/video/computer/video games), sleep duration, eating behavior, pros and cons of exercise, and exercise self-efficacy. According to the results, 45.7% of the children had screen time of 1-2.9 hr/day and 8.9% had 3 or more hr/day. Increased screen time showed an association with gender (boy), higher body mass index, fast food consumption, higher cons of exercise, having a working mother, and attendance at a school in an inner city area (p < .05). Understanding the factors associated with screen time may provide useful information in the development of health promotion programs aimed at decreasing sedentary behaviors. PMID:23598570

  4. Mean sojourn time and effectiveness of mortality reduction for lung cancer screening with computed tomography.

    PubMed

    Chien, Chun-Ru; Chen, Tony Hsiu-Hsi

    2008-06-01

    This study aimed to estimate the mean sojourn time (MST) and sensitivity of asymptomatic lung cancer (ALC) detected by computed tomography (CT) or chest X-ray (CXR). Translation of early diagnosis into mortality reduction by 2 detection modalities and inter-screening interval was projected using a Markov model. On the basis of systematic literature review, data from 6 prospective CT screening studies were retrieved. The MST in association with the natural history of lung cancer depicted by a 3-state Markov model was estimated with a Bayesian approach. To project mortality reduction attributed to screening, the model was further extended to 5 health states for the inclusion of prognostic part. The analysis was run with a 10-year time horizon of follow-up, mimicking the Dutch-Belgian randomized lung cancer screening trial (NELSON). Screening for lung cancer with CT had high sensitivity (median: 97%) and may advance 1 year earlier than CXR in detecting ALC. By simulating the scenario similar to NELSON study, CT screen may gain an extra of 0.019 year of life expectancy per person, yields 15% mortality reduction (relative risk (RR): 0.85, 95% confidence interval [95%CI: (0.58-1.01)]. Approximate 23% [RR: 0.77, 95%CI: (0.43-0.98)] mortality reduction would be achieved by annual CT screening program. The mortality findings in conjunction with higher sensitivity and shorter MST estimate given data on prevalent and incident (2nd) screen may provide a tentative evidence, suggesting that annual CT screening may be required in order to be effective in reducing mortality before the results of randomized controlled studies available. PMID:18302157

  5. A Nationwide Survey on the Daily Screen Time of Iranian Children and Adolescents: The CASPIAN - IV Study

    PubMed Central

    Jari, Mohsen; Qorbani, Mostafa; Motlagh, Mohammad Esmaeil; Heshmat, Ramin; Ardalan, Gelayol; Kelishadi, Roya

    2014-01-01

    Background: Leisure time activity is an important life-style habit. This study aims to determine the screen time of a nationally representative sample of Iranian children and adolescents. Methods: This nationwide cross-sectional study was conducted as part of the fourth survey of a surveillance system. The participants consisted of 14880 students, with aged range from 6 to 18 years, living in 30 provinces in Iran. Screen time, i.e. the time spent on watching television (TV)/video and computer games during leisure time, was assessed by using the questionnaire of the Globasl Student Health Survey of the World Health Organization. Results: The study participants were 13486 school students (participation rate of 90.6%) with a mean age of 12. 47 (3.36) years. Overall, 75.6% of students were from urban and 24.4% from rural areas and 50.8% were boys respectively. Overall, 33.4% and 53% of students watched TV/video more than 2 h a day in their leisure time during school days and holidays, respectively. Likewise, 6.3% and 10.9% of students used computer more than 2 h a day in their leisure time during the school days and holidays, respectively. Overall, 47.1% of urban students and 24.2% of rural students used personal computer in their leisure time during the school days. The corresponding figures were 50.8% and 27.2% in weekends and holidays, respectively. Conclusions: The time spent on screen activities is long in a considerably high number of Iranian children and adolescents. It should be reduced by increasing the public awareness and by providing facilities for regular daily physic activity for students’ leisure times. PMID:24627751

  6. Social-Cognitive Predictors of Low-Income Parents' Restriction of Screen Time among Preschool-Aged Children

    ERIC Educational Resources Information Center

    Lampard, Amy M.; Jurkowski, Janine M.; Davison, Kirsten K.

    2013-01-01

    Parents' rules regarding child television, DVD, video game, and computer use (screen time) have been associated with lower screen use in children. This study aimed to identify modifiable correlates of this behavior by examining social-cognitive predictors of parents' restriction of child screen time. Low-income parents ("N" =…

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

    PubMed

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

    2012-12-01

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

  8. Reconstruction of burst activity from calcium imaging of neuronal population via Lq minimization and interval screening

    PubMed Central

    Quan, Tingwei; Lv, Xiaohua; Liu, Xiuli; Zeng, Shaoqun

    2016-01-01

    Calcium imaging is becoming an increasingly popular technology to indirectly measure activity patterns in local neuronal networks. Based on the dependence of calcium fluorescence on neuronal spiking, two-photon calcium imaging affords single-cell resolution of neuronal population activity. However, it is still difficult to reconstruct neuronal activity from complex calcium fluorescence traces, particularly for traces contaminated by noise. Here, we describe a robust and efficient neuronal-activity reconstruction method that utilizes Lq minimization and interval screening (IS), which we refer to as LqIS. The simulation results show that LqIS performs satisfactorily in terms of both accuracy and speed of reconstruction. Reconstruction of simulation and experimental data also shows that LqIS has advantages in terms of the recall rate, precision rate, and timing error. Finally, LqIS is demonstrated to effectively reconstruct neuronal burst activity from calcium fluorescence traces recorded from large-size neuronal population. PMID:27375930

  9. Screen-time Weight-loss Intervention Targeting Children at Home (SWITCH): A randomized controlled trial study protocol

    PubMed Central

    2011-01-01

    Background Approximately one third of New Zealand children and young people are overweight or obese. A similar proportion (33%) do not meet recommendations for physical activity, and 70% do not meet recommendations for screen time. Increased time being sedentary is positively associated with being overweight. There are few family-based interventions aimed at reducing sedentary behavior in children. The aim of this trial is to determine the effects of a 24 week home-based, family oriented intervention to reduce sedentary screen time on children's body composition, sedentary behavior, physical activity, and diet. Methods/Design The study design is a pragmatic two-arm parallel randomized controlled trial. Two hundred and seventy overweight children aged 9-12 years and primary caregivers are being recruited. Participants are randomized to intervention (family-based screen time intervention) or control (no change). At the end of the study, the control group is offered the intervention content. Data collection is undertaken at baseline and 24 weeks. The primary trial outcome is child body mass index (BMI) and standardized body mass index (zBMI). Secondary outcomes are change from baseline to 24 weeks in child percentage body fat; waist circumference; self-reported average daily time spent in physical and sedentary activities; dietary intake; and enjoyment of physical activity and sedentary behavior. Secondary outcomes for the primary caregiver include change in BMI and self-reported physical activity. Discussion This study provides an excellent example of a theory-based, pragmatic, community-based trial targeting sedentary behavior in overweight children. The study has been specifically designed to allow for estimation of the consistency of effects on body composition for Māori (indigenous), Pacific and non-Māori/non-Pacific ethnic groups. If effective, this intervention is imminently scalable and could be integrated within existing weight management programs. Trial

  10. A Computational Methodology to Screen Activities of Enzyme Variants

    PubMed Central

    Hediger, Martin R.; De Vico, Luca; 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 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. PMID:23284627

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

    PubMed

    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)<30 micro g/ml in the DPPH radical reduction assay and IC(50)<32 micro g/ml in lipid peroxidation inhibition testing. Pimenta dioica and Curcuma longa L. showed also a 20% inhibition of the in vitro induced z.rad;OH attack to deoxyglucose. Further antimutagenesis assay in Escherichia coli IC 188 evidenced that only Pimenta dioica prevents DNA damage by TBH to the test bacteria. A role of antioxidant enzymes is presumed in this case, as judged by a different response in the isogenic Escherichia coli IC 203 deficient in catalase and alkyl hydroperoxide reductase and the discrete inhibition of oxidative mutagenesis also observed when pre-treatment of the extract was assayed. Eugenol, the main constituent of the essential oil of Pimenta dioica, also inhibited oxidative mutagenesis by TBH in Escherichia coli, at concentrations ranging from 150 to 400 micro g/plate. PMID:12860316

  12. The Leisure-Time Activity of Citizens

    ERIC Educational Resources Information Center

    Sedova, N. N.

    2011-01-01

    Survey data show that Russians relegate free time and leisure activity to secondary status compared to work, and free time faces the threat of becoming devalued and losing its importance as a life value. At the same time, in the structure of Russians' leisure activities there is an ongoing tendency for leisure to become simpler, for active types…

  13. Willingness-to-Pay to Avoid the Time Spent and Discomfort Associated with Screening Colonoscopy

    PubMed Central

    Jonas, Daniel E.; Russell, Louise B.; Chou, Jon; Pignone, Michael

    2014-01-01

    Background The screening colonoscopy process requires a considerable amount of time and some discomfort for patients. Objective We sought to use willingness-to-pay (WTP) to value the time required and the discomfort associated with screening colonoscopy. In addition, we aimed to explore some of the differences between and potential uses of the WTP and the human capital methods. Methods Subjects completed a diary recording time and a questionnaire including WTP questions to value the time and discomfort associated with colonoscopy. We also valued the elapsed time reported in the diaries (but not the discomfort) using the human capital method. Results 110 subjects completed the study. Mean WTP to avoid the time and discomfort was $263. Human capital values for elapsed time were greater. Linear regressions showed that WTP was influenced most by the difficulty of the preparation, which added $147 to WTP (p=0.03). Conclusions WTP values to avoid the time and discomfort associated with the screening colonoscopy process were substantially lower than most of the human capital values for elapsed time alone. The human capital method may overestimate the value of time in situations that involve an irregular, episodic series of time intervals, such as preparation for or recovery after colonoscopy. PMID:19725018

  14. Optimal timing in screening patients with congestive heart failure and healthy subjects during circadian observation.

    PubMed

    Jong, Tai-Lang; Chang, Ben; Kuo, Cheng-Deng

    2011-02-01

    Congestive heart failure (CHF) is a major medical challenge in developed countries. In order to screen patients with CHF and healthy subjects during circadian observation, accurate judgment and fast response are imperative. In this study, optimal timing during circadian observation via the heart rate variability (HRV) was sought. We tested 29 CHF patients and 54 healthy subjects in the control group from the interbeat interval databases of PhysioBank. By invoking the α1 parameter in detrended fluctuation analysis of HRV, we found that it could be used as an indicator to screen the patients with CHF and subjects in normal sinus rhythm (NSR) under Kruskal-Wallis test. By invoking Fano factor, the optimal timing to screen CHF patients and healthy subjects was found to be from 7 PM to 9 PM during the circadian observation. In addition, this result is robust in a sense that the same result can be achieved by using different ECG recording lengths of 2, 5, 10, … , and 120 min, respectively. Furthermore, a support vector machine was employed to classify CHF and NSR with α1 parameter of a moving half-hour ECG recordings via leave-one-out cross validation. The results showed that the superlative screening performance was obtained in the 7 pm-9 pm period during circadian observation. It is believed that this result of optimal timing will be helpful in the non-invasive monitoring and screening of CHF patients and healthy subjects in the clinical practice. PMID:20953708

  15. Developing a QSAR model for hepatotoxicity screening of the active compounds in traditional Chinese medicines.

    PubMed

    Huang, Shan-Han; Tung, Chun-Wei; Fülöp, Ferenc; Li, Jih-Heng

    2015-04-01

    The perception that natural substances are deemed safe has made traditional Chinese medicine (TCM) popular in the treatment and prevention of disease globally. However, such an assumption is often misleading owing to a lack of scientific validation. To assess the safety of TCM, in silico screening provides major advantages over the classical laboratory approaches in terms of resource- and time-saving and full reproducibility. To screen the hepatotoxicity of the active compounds of TCMs, a quantitative structure-activity relationship (QSAR) model was firstly established by utilizing drugs from the Liver Toxicity Knowledge Base. These drugs were annotated with drug-induced liver injury information obtained from clinical trials and post-marketing surveillance. The performance of the model after nested 10-fold cross-validation was 79.1%, 91.2%, 53.8% for accuracy, sensitivity, and specificity, respectively. The external validation of 91 well-known ingredients of common herbal medicines yielded a high accuracy (87%). After screening the TCM Database@Taiwan, the world's largest TCM database, a total of 6853 (74.8%) ingredients were predicted to have hepatotoxic potential. The one-hundred chemical ingredients predicted to have the highest hepatotoxic potential by our model were further verified by published literatures. Our study indicated that this model can serve as a complementary tool to evaluate the safety of TCM. PMID:25660478

  16. Physical activity and awareness in breast screening attendees in Black Country, UK.

    PubMed

    Lahart, Ian M; Reichl, Claire; Metsios, George S; Nevill, Alan M; Carmichael, Amtul R

    2016-03-01

    This study aimed to determine the physical activity levels and awareness of the influence of physical activity and overweight/obesity on breast cancer risk among NHS breast screening programme (NHSBSP) attendees. One hundred and eighty-eight (white British = 95%; post-menopausal = 80%) attendees completed a demographic and anthropometric data questionnaire, International Physical Activity Questionnaire (IPAQ) and awareness of breast cancer risk factors questionnaire. IPAQ data were reported as continuous measures (MET-min · week(-1)) and as categorical variables (low, moderate and high activities). The highest median physical activity levels were reported in the domestic physical activity domain (756 MET-min · week(-1)). Most participants were categorized as 'moderately active' (45%), while 30% were classified in the 'high activity' and 25% as 'low activity' categories. Almost a third of participants (30%) reported no leisure-time physical activity and 83% reported no vigorous physical activity. There was high awareness of the effects of physical activity (75%) and obesity (80%) on breast cancer risk. No significant differences were found between physical activity categories and awareness that physical activity can reduce breast cancer risk (p > 0.05). However, compared with moderate and high activity categories, participants in the 'low activity' category were significantly more likely to respond that they thought they achieved recommended physical activity levels (p < 0.05). Participants who are unaware of their inadequate physical activity levels may have a less positive intention to increase physical activity levels. Practical strategies aimed to increase knowledge of the recommended physical activity guidelines and facilitate the achievement of these guidelines may be required for NHSBSP attendees. PMID:25012881

  17. Screening of anticancer activity from agarwood essential oil

    PubMed Central

    Hashim, Yumi Zuhanis Has-Yun; Phirdaous, Abbas; Azura, Amid

    2014-01-01

    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 IC50 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 IC50 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. PMID:25002797

  18. Caffeine and Screen Time in Adolescence: Associations with Short Sleep and Obesity

    PubMed Central

    Drescher, Amy A.; Goodwin, James L.; Silva, Graciela E.; Quan, Stuart F.

    2011-01-01

    Objective: To investigate the associations between sleep duration and obesity incidence and risk factors among pre-adolescents and adolescents. Design: Cross-sectional study of a community based cohort Setting: The Tucson Children's Assessment of Sleep Apnea follow-up study (TuCASA) cohort. Participants: 319 Caucasian and Hispanics between 10-17 years. Main Outcome: Parent-reported sleep duration and BMI z-score. Outcome Measures: Surveys of electronic screen time, dietary and caffeine intake, exercise and sleep habits by parents, and anthropometric measures. Results: Parent-reported total sleep time (TST) was inversely associated with BMI z-score, but not significantly correlated with any of the examined nutritional variables or exercise components. Hispanic ethnicity was associated with significantly lower parent-reported TST and higher BMI z-score. Parent-reported TST was inversely related to electronic screen time and caffeine use, but these findings were differentially related to age. Caffeine consumption was associated with decreasing parent-reported TST primarily in older adolescents. Electronic screen time was associated with lower parent-reported TST in younger adolescents. Conclusions: Hispanic ethnicity and parental reports of TST were found to be the most closely associated with BMI z-score. Decreased TST and increased caffeine intake and screen time may result in higher obesity risk in the adolescent population. Citation: Drescher AA; Goodwin JL; Silva GE; Quan SF. Caffeine and screen time in adolescence: associations with short sleep and obesity. J Clin Sleep Med 2011;7(4):337-342. PMID:21897768

  19. Young Children and Screen Time: Creating a Mindful Approach to Digital Technology

    ERIC Educational Resources Information Center

    Neumann, Michelle Margaret

    2015-01-01

    To effectively address early childhood screen time concerns raised by parents and policy makers it is important to examine the current home digital environments of young children. The present study draws upon research that examined the home digital environment of Australian parents and their children (aged 2 to 4; N = 69). Parents completed a…

  20. Moving beyond Screen Time: Redefining Developmentally Appropriate Technology Use in Early Childhood Education. Policy Brief

    ERIC Educational Resources Information Center

    Daugherty, Lindsay; Dossani, Rafiq; Johnson, Erin-Elizabeth; Wright, Cameron

    2014-01-01

    Conversations about what constitutes "developmentally appropriate" use of technology in early childhood education have, to date, focused largely on a single, blunt measure--screen time--that fails to capture important nuances, such as what type of media a child is accessing and whether technology use is taking place solo or with peers.…

  1. Factors Associated with Screen Time among School-Age Children in Korea

    ERIC Educational Resources Information Center

    Ham, Ok Kyung; Sung, Kyung Mi; Kim, Hee Kyung

    2013-01-01

    The purpose of this study was to investigate the association of sociodemographic, psychosocial, and behavioral characteristics with screen time among school-age children in Korea. This study employed a nonexperimental, cross-sectional study design. A total of 370 children attending four elementary schools participated in the study. Self-report…

  2. Some Effects of Row, Diagonal, and Column Screen Formats on Search Time and Strategy.

    ERIC Educational Resources Information Center

    Emurian, Henry H.; Seborg, Brian H.

    1990-01-01

    Describes a study of undergraduates that examined differences in computer screen formats and their effects on search time and strategy. Row, diagonal, and column information formats are compared, as well as tightly packed and loosely packed displays, and results of regression and residual analyses are discussed. (38 references) (LRW)

  3. Extending the Global Dialogue about Media, Technology, Screen Time, and Young Children

    ERIC Educational Resources Information Center

    Ernest, James M.; Causey, Cora; Newton, Allison B.; Sharkins, Kimberly; Summerlin, Jennifer; Albaiz, Najla

    2014-01-01

    Questions about the potential benefits and dangers of media and technology use abound, with competing theories regarding its effects among young children. This article explores global perspectives on children's exposure to media, technology, and screen time (MeTS) in the schools, homes, and communities of an increasingly technology-driven…

  4. Sedentary Time and Screen-Based Sedentary Behaviors of Children With a Chronic Disease.

    PubMed

    Walker, Rachel G; Obeid, Joyce; Nguyen, Thanh; Ploeger, Hilde; Proudfoot, Nicole A; Bos, Cecily; Chan, Anthony K; Pedder, Linda; Issenman, Robert M; Scheinemann, Katrin; Larché, Maggie J; McAssey, Karen; Timmons, Brian W

    2015-05-01

    The objectives of this study were to (i) assess sedentary time and prevalence of screen-based sedentary behaviors of children with a chronic disease and (ii) compare sedentary time and prevalence of screen-based sedentary behaviors to age- and sex-matched healthy controls. Sixty-five children (aged 6-18 years) with a chronic disease participated: survivors of a brain tumor, hemophilia, type 1 diabetes mellitus, juvenile idiopathic arthritis, cystic fibrosis, and Crohn's disease. Twenty-nine of these participants were compared with age- and sex-matched healthy controls. Sedentary time was measured objectively by an ActiGraph GT1M or GT3× accelerometer worn for 7 consecutive days and defined as less than 100 counts per min. A questionnaire was used to assess screen-based sedentary behaviors. Children with a chronic disease engaged in an average of 10.2 ± 1.4 hr of sedentary time per day, which comprised 76.5 ± 7.1% of average daily monitoring time. There were no differences between children with a chronic disease and controls in sedentary time (adjusted for wear time, p = .06) or in the prevalence of TV watching, and computer or video game usage for varying durations (p = .78, p = .39 and, p = .32 respectively). Children with a chronic disease, though relatively healthy, accumulate high levels of sedentary time, similar to those of their healthy peers. PMID:25389217

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

    PubMed

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

    2015-04-01

    Due to major problems with drug resistance in parasitic nematodes of animals, there is a substantial need and excellent opportunities to develop new anthelmintics via genomic-guided and/or repurposing approaches. In the present study, we established a practical and cost-effective whole-organism assay for the in vitro-screening of compounds for activity against parasitic stages of the nematode Haemonchus contortus (barber's pole worm). The assay is based on the use of exsheathed L3 (xL3) and L4 stages of H. contortus of small ruminants (sheep and goats). Using this assay, we screened a panel of 522 well-curated kinase inhibitors (GlaxoSmithKline, USA; code: PKIS2) for activity against H. contortus by measuring the inhibition of larval motility using an automated image analysis system. We identified two chemicals within the compound classes biphenyl amides and pyrazolo[1,5-α]pyridines, which reproducibly inhibit both xL3 and L4 motility and development, with IC50s of 14-47 μM. Given that these inhibitors were designed as anti-inflammatory drugs for use in humans and fit the Lipinski rule-of-five (including bioavailability), they show promise for hit-to-lead optimisation and repurposing for use against parasitic nematodes. The screening assay established here has significant advantages over conventional methods, particularly in terms of ease of use, throughput, time and cost. Although not yet fully automated, the current assay is readily suited to the screening of hundreds to thousands of compounds for subsequent hit-to-lead optimisation. The current assay is highly adaptable to many parasites of socioeconomic importance, including those causing neglected tropical diseases. This aspect is of major relevance, given the urgent need to deliver the goals of the London Declaration (http://unitingtocombatntds.org/resource/london-declaration) through the rapid and efficient repurposing of compounds in public-private partnerships. PMID:25746136

  6. Vocal Activity, Time Pressure and Interpersonal Judgments.

    ERIC Educational Resources Information Center

    Daly, John A.; Lashbrook, William B.

    This study examined the effects of differential time pressures on small group members' rankings of one another based on vocal activity. Vocal activity was operationalized as observed frequency of interaction. Time pressure was manipulated by allowing either six minutes or no time limit on a group problem-solving task. Main effects were…

  7. Environmental measurement while drilling system for real-time field screening of contaminants

    SciTech Connect

    Williams, C.V.; Lockwood, G.J.; Normann, R.A.

    1996-12-31

    Sampling during environmental drilling is essential to fully characterize the spatial distribution and migration of subsurface contaminants. Real-time information on environmental conditions, drill bit location and temperature during drilling is valuable in many environmental restoration operations. This type of information can be used to provide field screening data and improved efficiency of site characterization activities. The Environmental Measurement-While-Drilling (EMWD) System represents an innovative blending of new and existing technology in order to obtain real-time data during drilling. The system consists of two subsystems. The down-hole subsystem (at the drill bit) consists of sensors, a power supply, a signal conditioning and transmitter board, and a radio-frequency (RF) coaxial cable. The up-hole subsystem consists of a battery pack/coil, pickup coil, receiver, and personal computer. The system is compatible with fluid miser drill pipe, a directional drilling technique that uses minimal drilling fluids and generates little to no secondary waste. In EMWD, downhole sensors are located behind the drill bit and linked by a high-speed data transmission system to a computer at the surface. As drilling is conducted, data is collected on the nature and extent of contamination, enabling on-the-spot decisions regarding drilling and sampling strategies. Initially, the downhole sensor consisted of a simple gamma radiation detector, a Geiger-Mueller tube (GMT). The EMWD system has been improved by the integration of a Gamma Ray Spectrometer (GRS) in place of the GMT. The GRS consists of a sodium iodide-thallium activated crystal coupled to a photomultiplier tube (PMT). The output of the PMT goes to a multichannel analyzer (MCA). The MCA data is transmitted to the surface via a signal conditioning and transmitter board similar to that used with the GMT. The EMWD system is described and the results of the GRS field tests and field demonstration are presented.

  8. Impact of Co-Occurring Birth Defects on the Timing of Newborn Hearing Screening and Diagnosis

    PubMed Central

    Chapman, Derek A.; Stampfel, Caroline C.; Bodurtha, Joann N.; Dodson, Kelley M.; Pandya, Arti; Lynch, Kathleen B.; Kirby, Russell S.

    2016-01-01

    Purpose Early detection of hearing loss in all newborns and timely intervention are critical to children's cognitive, verbal, behavioral, and social development. The initiation of appropriate early intervention services before 6 months of age can prevent or reduce negative developmental consequences. The purpose of this study was to assess, using large, population-based registries, the effect of co-occurring birth defects (CBDs) on the timing and overall rate of hearing screening and diagnosis. Method The authors linked statewide data from newborn hearing screenings, a birth defects registry, and birth certificates to assess the timeliness of newborn hearing screening and diagnosis of hearing loss (HL) for infants with and without CBDs in 485 children with confirmed HL. Results Nearly one third (31.5%) of children with HL had 1 or more CBDs. The presence of CBDs prolonged the time of the initial infant hearing screening, which contributed to further delays in the subsequent diagnosis of HL. Conclusions Better coordination of HL assessment into treatment plans for children with CBDs may enable earlier diagnosis of HL and provide opportunities for intervention that will affect long-term developmental outcomes for these children. PMID:21940980

  9. Newborn screening of phenylketonuria using direct analysis in real time (DART) mass spectrometry.

    PubMed

    Wang, Chunyan; Zhu, Hongbin; Cai, Zongwei; Song, Fengrui; Liu, Zhiqiang; Liu, Shuying

    2013-04-01

    Phenylketonuria (PKU) is commonly included in the newborn screening panel of most countries, with various techniques being used for quantification of L-phenylalanine (Phe). To diagnose PKU as early as possible in newborn screening, a rapid and simple method of analysis was developed. Using direct analysis in real time (DART) ionization coupled with triple-quadrupole tandem mass spectrometry (TQ-MS/MS) and with use of a 12 DIP-it tip scanner autosampler in positive ion mode, we analyzed dried blood spot (DBS) samples from PKU newborns. The concentration of Phe was determined using multiple reaction monitoring mode with the nondeuterated internal standard N,N-dimethylphenylalanine. The results of the analysis of DBS samples from newborns indicated that the DART-TQ-MS/MS method is fast, accurate, and reproducible. The results prove that this assay as a newborn screen for PKU can be performed in 18 s per sample for the quantification of Phe in DBS samples. DART-TQ-MS/MS analysis of the Phe concentration in DBS samples allowed us to screen newborns for PKU. This innovative protocol is rapid and can be effectively applied on a routine basis to analyze a large number of samples in PKU newborn screening and PKU patient monitoring. PMID:23397086

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

    PubMed

    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. PMID:27166668

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

    PubMed

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

    2013-05-23

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

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

    PubMed Central

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

    2013-01-01

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

  13. Computational reverse chemical ecology: Virtual screening and predicting behaviorally active semiochemicals for Bactrocera dorsalis

    PubMed Central

    2014-01-01

    Background Semiochemical is a generic term used for a chemical substance that influences the behaviour of an organism. It is a common term used in the field of chemical ecology to encompass pheromones, allomones, kairomones, attractants and repellents. Insects have mastered the art of using semiochemicals as communication signals and rely on them to find mates, host or habitat. This dependency of insects on semiochemicals has allowed chemical ecologists to develop environment friendly pest management strategies. However, discovering semiochemicals is a laborious process that involves a plethora of behavioural and analytical techniques, making it expansively time consuming. Recently, reverse chemical ecology approach using odorant binding proteins (OBPs) as target for elucidating behaviourally active compounds is gaining eminence. In this scenario, we describe a “computational reverse chemical ecology” approach for rapid screening of potential semiochemicals. Results We illustrate the high prediction accuracy of our computational method. We screened 25 semiochemicals for their binding potential to a GOBP of B. dorsalis using molecular docking (in silico) and molecular dynamics. Parallely, compounds were subjected to fluorescent quenching assays (Experimental). The correlation between in silico and experimental data were significant (r2 = 0.9408; P < 0.0001). Further, predicted compounds were subjected to behavioral bioassays and were found to be highly attractive to insects. Conclusions The present study provides a unique methodology for rapid screening and predicting behaviorally active semiochemicals. This methodology may be developed as a viable approach for prospecting active semiochemicals for pest control, which otherwise is a laborious process. PMID:24640964

  14. An Actor-Based Model of Social Network Influence on Adolescent Body Size, Screen Time, and Playing Sports

    PubMed Central

    Shoham, David A.; Tong, Liping; Lamberson, Peter J.; Auchincloss, Amy H.; Zhang, Jun; Dugas, Lara; Kaufman, Jay S.; Cooper, Richard S.; Luke, Amy

    2012-01-01

    Recent studies suggest that obesity may be “contagious” between individuals in social networks. Social contagion (influence), however, may not be identifiable using traditional statistical approaches because they cannot distinguish contagion from homophily (the propensity for individuals to select friends who are similar to themselves) or from shared environmental influences. In this paper, we apply the stochastic actor-based model (SABM) framework developed by Snijders and colleagues to data on adolescent body mass index (BMI), screen time, and playing active sports. Our primary hypothesis was that social influences on adolescent body size and related behaviors are independent of friend selection. Employing the SABM, we simultaneously modeled network dynamics (friendship selection based on homophily and structural characteristics of the network) and social influence. We focused on the 2 largest schools in the National Longitudinal Study of Adolescent Health (Add Health) and held the school environment constant by examining the 2 school networks separately (N = 624 and 1151). Results show support in both schools for homophily on BMI, but also for social influence on BMI. There was no evidence of homophily on screen time in either school, while only one of the schools showed homophily on playing active sports. There was, however, evidence of social influence on screen time in one of the schools, and playing active sports in both schools. These results suggest that both homophily and social influence are important in understanding patterns of adolescent obesity. Intervention efforts should take into consideration peers’ influence on one another, rather than treating “high risk” adolescents in isolation. PMID:22768124

  15. A microscale platform for integrated cell-free expression and activity screening of cellulases.

    PubMed

    Chandrasekaran, Aarthi; Bharadwaj, Rajiv; Park, Joshua I; Sapra, Rajat; Adams, Paul D; Singh, Anup K

    2010-11-01

    Recent advances in production of cellulases by genetic engineering and isolation from natural microbial communities have necessitated the development of high-throughput analytical technologies for cellulase expression and screening. We have developed a novel cost-effective microscale approach based on in vitro protein synthesis, which seamlessly integrates cellulase expression with activity screening without the need for any protein purification procedures. Our platform achieves the entire process of transcription, translation, and activity screening within 2-3 hours in microwell arrays compared with days needed for conventional cell-based cellulase expression, purification, and activity screening. Highly sensitive fluorescence-based detection permits activity screening in volumes as low as 2-3 μL with minimal evaporation (even at temperatures as high as 95 °C) leading to two orders of magnitude reduction in reagent usage and cost. The platform was used for rapid expression and screening of β-glucosidases (BGs) and cellobiohydrolases (CBHs) isolated from thermophilic microorganisms. Furthermore, it was also used to determine optimum temperatures for BG and CBH activities and to study product inhibition of CBHs. The approach described here is well suited for first-pass screening of large libraries to identify cellulases with desired properties that can subsequently be produced on a large scale for detailed structural and functional characterization. PMID:20735086

  16. Development of quantitative duplex real-time PCR method for screening analysis of genetically modified maize.

    PubMed

    Oguchi, Taichi; Onishi, Mari; Minegishi, Yasutaka; Kurosawa, Yasunori; Kasahara, Masaki; Akiyama, Hiroshi; Teshima, Reiko; Futo, Satoshi; Furui, Satoshi; Hino, Akihiro; Kitta, Kazumi

    2009-06-01

    A duplex real-time PCR method was developed for quantitative screening analysis of GM maize. The duplex real-time PCR simultaneously detected two GM-specific segments, namely the cauliflower mosaic virus (CaMV) 35S promoter (P35S) segment and an event-specific segment for GA21 maize which does not contain P35S. Calibration was performed with a plasmid calibrant specially designed for the duplex PCR. The result of an in-house evaluation suggested that the analytical precision of the developed method was almost equivalent to those of simplex real-time PCR methods, which have been adopted as ISO standard methods for the analysis of GMOs in foodstuffs and have also been employed for the analysis of GMOs in Japan. In addition, this method will reduce both the cost and time requirement of routine GMO analysis by half. The high analytical performance demonstrated in the current study would be useful for the quantitative screening analysis of GM maize. We believe the developed method will be useful for practical screening analysis of GM maize, although interlaboratory collaborative studies should be conducted to confirm this. PMID:19602858

  17. A time-scale sensitometric method for evaluating screen-film systems.

    PubMed

    Góes, E G; Pelá, C A; Ghilardi, N T

    1997-10-01

    An x-ray sensitometer is used to measure the characteristic curve of radiographic films exposed with fluorescent intensifying screens. The series of relative exposures, necessary to cover the full density range of the film, can be obtained by either time-scale or intensity-scale sensitometric methods. We have developed a convenient method of exposing film-screen systems for time-scale sensitometry. In this method, during exposure the x-ray kilovoltage, tube current and x-ray intensity remain constant and a geometric series of exposures of the film is modulated by varying the exposure time. This time variation can be obtained when a lead disc with different sector openings is rotated in front of the film system by a stepping motor. The conditions normally used are 70 kVp x-rays, 3.5 mm Al total filtration at the tube, and 2.4 m focal spot-film distance. This exposure latitude gives a complete characteristic curve of film-screen systems. PMID:9364589

  18. A time-scale sensitometric method for evaluating screen - film systems

    NASA Astrophysics Data System (ADS)

    Góes, E. G.; Pelá, C. A.; Ghilardi, Netto T.

    1997-10-01

    An x-ray sensitometer is used to measure the characteristic curve of radiographic films exposed with fluorescent intensifying screens. The series of relative exposures, necessary to cover the full density range of the film, can be obtained by either time-scale or intensity-scale sensitometric methods. We have developed a convenient method of exposing film - screen systems for time-scale sensitometry. In this method, during exposure the x-ray kilovoltage, tube current and x-ray intensity remain constant and a geometric series of exposures of the film is modulated by varying the exposure time. This time variation can be obtained when a lead disc with different sector openings is rotated in front of the film system by a stepping motor. The conditions normally used are 70 kVp x-rays, 3.5 mm Al total filtration at the tube, and 2.4 m focal spot - film distance. This exposure latitude gives a complete characteristic curve of film - screen systems.

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

    PubMed

    Chen, B; Zhuo, W

    2015-11-01

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

  20. PFA-100 closure times in preoperative screening in 500 pediatric patients.

    PubMed

    Roschitz, Birgit; Thaller, Sigrid; Koestenberger, Martin; Wirnsberger, Andrea; Leschnik, Bettina; Fritsch, Peter; Muntean, Wolfgang

    2007-07-01

    Three to five percent of patients undergoing surgery have either an acquired or congenital platelet defect or von Willebrand disease (vWD). The predictive value of preoperative coagulation screening is questionable. PFA-100 is now routinely used in preoperative screening in our pediatric outpatient service. We wanted to assess whether the PFA-100 would help to identify patients with primary haemostatic defects or if the additional use of PFA-100 would add to the problem of unnecessary pathologic preoperative laboratory values resulting in delay of surgical procedure. We investigated 500 children consecutively seen in our outpatient service before surgery. Blood cell count, aPTT, PFA-100 closure times (CT) were done in all patients. If abnormalities were found, the patient was presented to a haemostatic expert. vWF:AG, R:Cof and factor VIII were analysed in all patients with prolonged closure times and APTT values. One hundred twenty-six patients (25.2%) showed abnormalities in APTT and/or PFA-100. Further investigations in 89 of these 126 patients did not yield a specific diagnosis; neither diagnostic criteria for impaired haemostasis were found by questionnaire. None of these 89 patients had a bleeding complication during surgery. Forty-eight patients showed prolonged CTs. Twelve patients with low vWF:AG were detected, 10 of these patients were found by PFA-100. Four of these patients did present with normal APTT values. Our study shows that similar to the APTT the PFA-100 is probably only a good screening method when a haemostatic defect in a patient is clinically likely, especially to screen forVWD, and the test should not be used in general unselective screening. PMID:17598019

  1. Environmental Measurement-While-Drilling System for Real-Time Field Screening of Contaminants

    SciTech Connect

    Bishop, L.B.; Lockwood, G.J.; Normann, R.A.; Selph, M.M.; Williams, C.V.

    1999-02-22

    Sampling during environmental drilling is essential to fully characterize the spatial distribution and migration of near surface contaminants. However, analysis of the samples is expensive and time-consuming: off-site laboratory analysis can take weeks or months. An alternative screening technology, Environmental Measurement-While-Drilling (EMWD), could save money and valuable time by quickly distinguishing between contaminated and uncontaminated areas. Real time measurements provided by an EMWD system enable on-the-spot decisions to be made regarding sampling strategies. The system also enhances worker safety and provides the added flexibility of being able to steer a drill bit in or out of hazardous zones.

  2. Environmental Measurement While Drilling System for Real-Time Field Screening of Contaminants

    SciTech Connect

    Lockwood, G.J.; Normann, R.A.; Williams, C.V.

    1999-02-22

    Sampling during environmental drilling is essential to fully characterize the spatial distribution and migration of subsurface contaminants. However, analysis of the samples is expensive and time-consuming: off-site laboratory analysis can take weeks or months. Real-time information on environmental conditions, drill bit location and temperature during drilling is valuable in many environmental restoration operations. This type of information can be used to provide field screening data and improved efficiency of site characterization activities. The Environmental Measurement-While-Drilling (EMWD) System represents an innovative blending of new and existing technology in order to obtain real-time data during drilling. The system consists of two subsystems. The down-hole subsystem (at the drill bit) consists of sensors, a power supply, a signal conditioning and transmitter board, and a radio-frequency (RF) coaxial cable. The up-hole subsystem consists of a battery pack/coil, pickup coil, receiver, and personal computer. The system is compatible with fluid miser drill pipe, a directional drilling technique that uses minimal drilling fluids and generates little to no secondary waste. In EMWD, downhole sensors are located behind the drill bit and linked by a high-speed data transmission system to a computer at the surface. Sandia-developed Windows{trademark}-based software is used for data display and storage. As drilling is conducted, data is collected on the nature and extent of contamination, enabling on-the-spot decisions regarding drilling and sampling strategies. Initially, the downhole sensor consisted of a simple gamma radiation detector, a Geiger-Mueller tube (GMT). The design includes data assurance techniques to increase safety by reducing the probability of giving a safe indication when an unsafe condition exists. The EMWD system has been improved by the integration of a Gamma Ray Spectrometer (GRS) in place of the GMT. The GRS consists of a sodium iodide

  3. Chemical Composition Analysis, Antimicrobial Activity and Cytotoxicity Screening of Moss Extracts (Moss Phytochemistry).

    PubMed

    Klavina, Laura; Springe, Gunta; Nikolajeva, Vizma; Martsinkevich, Illia; Nakurte, Ilva; Dzabijeva, Diana; Steinberga, Iveta

    2015-01-01

    Mosses have been neglected as a study subject for a long time. Recent research shows that mosses contain remarkable and unique substances with high biological activity. The aim of this study, accordingly, was to analyze the composition of mosses and to screen their antimicrobial and anticancer activity. The total concentration of polyphenols and carbohydrates, the amount of dry residue and the radical scavenging activity were determined for a preliminary evaluation of the chemical composition of moss extracts. In order to analyze and identify the substances present in mosses, two types of extrahents (chloroform, ethanol) and the GC/MS and LC-TOF-MS methods were used. The antimicrobial activity was tested on four bacteria strains, and the anticancer activity on six cancer cell lines. The obtained results show the presence of a high number of primary (fatty acids and amino acids), but mainly secondary metabolites in moss extracts-including, sterols, terpenoids, polyphenols and others-and a high activity with respect to the studied test organisms. PMID:26393559

  4. Quantification and clustering of phenotypic screening data using time-series analysis for chemotherapy of schistosomiasis

    PubMed Central

    2012-01-01

    Background Neglected tropical diseases, especially those caused by helminths, constitute some of the most common infections of the world's poorest people. Development of techniques for automated, high-throughput drug screening against these diseases, especially in whole-organism settings, constitutes one of the great challenges of modern drug discovery. Method We present a method for enabling high-throughput phenotypic drug screening against diseases caused by helminths with a focus on schistosomiasis. The proposed method allows for a quantitative analysis of the systemic impact of a drug molecule on the pathogen as exhibited by the complex continuum of its phenotypic responses. This method consists of two key parts: first, biological image analysis is employed to automatically monitor and quantify shape-, appearance-, and motion-based phenotypes of the parasites. Next, we represent these phenotypes as time-series and show how to compare, cluster, and quantitatively reason about them using techniques of time-series analysis. Results We present results on a number of algorithmic issues pertinent to the time-series representation of phenotypes. These include results on appropriate representation of phenotypic time-series, analysis of different time-series similarity measures for comparing phenotypic responses over time, and techniques for clustering such responses by similarity. Finally, we show how these algorithmic techniques can be used for quantifying the complex continuum of phenotypic responses of parasites. An important corollary is the ability of our method to recognize and rigorously group parasites based on the variability of their phenotypic response to different drugs. Conclusions The methods and results presented in this paper enable automatic and quantitative scoring of high-throughput phenotypic screens focused on helmintic diseases. Furthermore, these methods allow us to analyze and stratify parasites based on their phenotypic response to drugs

  5. Toxicology screen

    MedlinePlus

    Barbiturates - screen; Benzodiazepines - screen; Amphetamines - screen; Analgesics - screen; Antidepressants - screen; Narcotics - screen; Phenothiazines - screen; Drug abuse screen; Blood alcohol test

  6. Time-trend of melanoma screening practice by primary care physicians: A meta-regression analysis

    PubMed Central

    Mauri, Davide; Karampoiki, Vassiliki; Polyzos, Nikolaos P; Cortinovis, Ivan; Koukourakis, Georgios; Zacharias, Georgios; Xilomenos, Apostolos; Tsappi, Maria; Casazza, Giovanni

    2009-01-01

    Objective To assess whether the proportion of primary care physicians implementing full body skin examination (FBSE) to screen for melanoma changed over time. Methods Meta-regression analyses of available data. Data Sources: MEDLINE, ISI, Cochrane Central Register of Controlled Trials. Results Fifteen studies surveying 10,336 physicians were included in the analyses. Overall, 15%–82% of them reported to perform FBSE to screen for melanoma. The proportion of physicians using FBSE screening tended to decrease by 1.72% per year (P =0.086). Corresponding annual changes in European, North American, and Australian settings were −0.68% (P =0.494), −2.02% (P =0.044), and +2.59% (P =0.010), respectively. Changes were not influenced by national guide-lines. Conclusions Considering the increasing incidence of melanoma and other skin malignancies, as well as their relative potential consequences, the FBSE implementation time-trend we retrieved should be considered a worrisome phenomenon. PMID:19242870

  7. Real-Time Monitoring of Active Landslides

    USGS Publications Warehouse

    Reid, Mark E.; LaHusen, Richard G.; Ellis, William L.

    1999-01-01

    Landslides threaten lives and property in every State in the Nation. To reduce the risk from active landslides, the U.S. Geological Survey (USGS) develops and uses real-time landslide monitoring systems. Monitoring can detect early indications of rapid, catastrophic movement. Up-to-the-minute or real-time monitoring provides immediate notification of landslide activity, potentially saving lives and property. Continuous information from real-time monitoring also provides a better understanding of landslide behavior, enabling engineers to create more effective designs for halting landslide movement.

  8. A home sleep apnea screening device with time-domain signal processing and autonomous scoring capability.

    PubMed

    Jin, Jiayi; Sánchez-Sinencio, Edgar

    2015-02-01

    Current solutions of sleep apnea diagnosis require the patient to undergo overnight studies at a specialized sleep laboratory. Due to such inconvenience and high cost, millions of sleep apnea patients remain undiagnosed and thus untreated. Based on a micro-electro-mechanical systems (MEMS) sensor and an effective apnea detection algorithm, we propose a low-cost single-channel apnea screening solution applicable in the comfort of patients' homes. A prototype device was designed and assembled including a MEMS sensor for measuring the patient's nasal air flows, and a time-domain signal processing IC for apnea detection and autonomous scoring. The IC chip was fabricated in standard 0.5- μm CMOS technology. The proposed device was tested for both respiratory rhythm detection and sleep apnea screening under clinical environment. Apnea-hypopnea indices (AHI) were scored to indicate severity of sleep apnea conditions. Test results suggest that the proposed device can be a valuable screening solution for the broader public with undiagnosed apnea conditions. PMID:25486649

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

    PubMed

    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

    2015-06-01

    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

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

    PubMed Central

    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

  11. Screening the Hemostatic Active Fraction of Artemisia annua L. In-vitro

    PubMed Central

    Wang, Bochu; Sui, Jing; Yu, Zhengwen; Zhu, Liancai

    2011-01-01

    Artemisinin extracted from Artemisia annua L. is the best medicine with the highest efficiency, the most effective and the lowest toxicity in treating ague nowadays. At present, most studies focus on artemisinin and its derivatives, while the study and report about the other active components are rare. This paper purposed to further discover new indication of Artemisia annua L. connecting with the record of traditional medicine. We screened the hemostatic active fraction of Artemisia annua L. in-vitro by plasma recalcification time (PRT). The crude extract and the extract of n-butanol were purified by polyamide, MCI, gel column in order. Determining the part of 20% methanol fraction after column chromatography of MCI gel is the hemostatic active fraction of Artemisia annua L. The shorten rate of clotting time are followed by: crude extract of Artemisin annua L. (8.51%); the n-butanol extract (14.89%); water eluting fraction after the extract of n-butanol was purificated by polyamide (22.11%); 20% methanol fraction after column chromatography of MCI gel (27.37%). It can provide experimental data for the clinical application of Artemisia annua L. which can be exploited as hemostatic. This topic has a certain academic value and potential prospects on the deep research of the Artemisia annua L. resource. PMID:24363681

  12. Mouse Activity across Time Scales: Fractal Scenarios

    PubMed Central

    Lima, G. Z. dos Santos; Lobão-Soares, B.; do Nascimento, G. C.; França, Arthur S. C.; Muratori, L.; Ribeiro, S.; Corso, G.

    2014-01-01

    In this work we devise a classification of mouse activity patterns based on accelerometer data using Detrended Fluctuation Analysis. We use two characteristic mouse behavioural states as benchmarks in this study: waking in free activity and slow-wave sleep (SWS). In both situations we find roughly the same pattern: for short time intervals we observe high correlation in activity - a typical 1/f complex pattern - while for large time intervals there is anti-correlation. High correlation of short intervals ( to : waking state and to : SWS) is related to highly coordinated muscle activity. In the waking state we associate high correlation both to muscle activity and to mouse stereotyped movements (grooming, waking, etc.). On the other side, the observed anti-correlation over large time scales ( to : waking state and to : SWS) during SWS appears related to a feedback autonomic response. The transition from correlated regime at short scales to an anti-correlated regime at large scales during SWS is given by the respiratory cycle interval, while during the waking state this transition occurs at the time scale corresponding to the duration of the stereotyped mouse movements. Furthermore, we find that the waking state is characterized by longer time scales than SWS and by a softer transition from correlation to anti-correlation. Moreover, this soft transition in the waking state encompass a behavioural time scale window that gives rise to a multifractal pattern. We believe that the observed multifractality in mouse activity is formed by the integration of several stereotyped movements each one with a characteristic time correlation. Finally, we compare scaling properties of body acceleration fluctuation time series during sleep and wake periods for healthy mice. Interestingly, differences between sleep and wake in the scaling exponents are comparable to previous works regarding human heartbeat. Complementarily, the nature of these sleep-wake dynamics could lead to a better

  13. In vitro screening of leishmanicidal activity in myanmar timber extracts.

    PubMed

    Takahashi, Marii; Fuchino, Hiroyuki; Satake, Motoyoshi; Agatsuma, Yutaka; Sekita, Setsuko

    2004-06-01

    Seventy-five Myanmar timber extracts belonging to 27 families were examined for their leishmanicidal activities. Some timber extracts had significant leishmanicidal activity, especially extracts of Millettia pendula, which exhibited the most potent activity (MLC 3.1 microg/ml, MIC 1.6 microg/ml). Other timber extracts showing potent activity included those from Cedrela serrata, Cedrela toona, Cordia fragrantissima, Calophyllum kunstleri, Dalbergia cultrate, Grevillea robusta, Haplophragma adenophyllum, Michelia champaca, and Tectona grandis. From a literature search for reports on the chemical constituents of these plants, most constituents were found to be quinone derivatives or other compounds with unsaturated carbonyl groups. PMID:15187448

  14. Screening of traditionally used endemic Soqotraen plants for cytotoxic activity.

    PubMed

    Ali, Nasser A Awadh; Mothana, Ramzi; Ghaleb, Nasr Abdo; Lindequist, Ulrike

    2007-01-01

    Thirty extracts obtained from 10 endemic plant species belonging to 8 plant families used in the traditional medicine in Socotra have been tested for cytotoxic activity against FL-cells. Extracts of Eureiandra balfourii and Commiphora ornifolia showed the strongest activity against FL-cells with IC(50) < 10 microg/ml and 39.3 microg/ml respectively. PMID:20161922

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

    PubMed Central

    Vats, Manisha; Singh, Harneet; Sardana, Satish

    2011-01-01

    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. PMID:24031791

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

    PubMed Central

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

    2011-01-01

    Objective: Coriandrum sativum (Linn.), a glabrous, aromatic, herbaceous annual plant, is well known for its use in jaundice. Essential oil, flavonoids, fatty acids, and sterols have been isolated from different parts of C. sativum. The plant has a very effective antioxidant profile showing 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, lipoxygenase inhibition, phospholipid peroxidation inhibition, iron chelating activity, hydroxyl radical scavenging activity, superoxide dismutation, glutathione reduction and antilipid peroxidation due to its high total phenolic content with the presence of constituents like pyrogallol, caffeic acid, glycitin, etc. Materials and Methods: This study was aimed at investigating the hepatoprotective activity of C. sativum against carbon tetrachloride (CCl4), with estimation of serum serum glutamyl oxaloacetic acid transaminase (SGOT), serum glutamyl pyruvate transaminase (SGPT), alkaine phosphatase (ALP) and bilirubin, and with liver histopathology. Results: Ethanolic extract was found to be rich in alkaloids, phenolic compounds and flavonoids, and high performance liquid chromatography (HPLC) fingerprinting showed the presence of iso-quercetin and quercetin. C. sativum signifies hepatoprotection by reducing the liver weight, activities of SGOT, SGPT, and ALP, and direct bilirubin of CCl4 intoxicated animals. Administration of C. sativum extract at 300 mg/kg dose resulted in disappearance of fatty deposit, ballooning degeneration and necrosis, indicating antihepatotoxic activity. Conclusion: The results of this study have led to the conclusion that ethanolic extract of C. sativum possesses hepatoprotective activity which may be due to the antioxidant potential of phenolic compounds. PMID:21966166

  17. Barriers to Screening and Possibilities for Active Detection of Family Medicine Attendees Exposed to Intimate Partner Violence

    PubMed Central

    KOPČAVAR GUČEK, Nena; PETEK, Davorina; ŠVAB, Igor; SELIČ, Polona

    2016-01-01

    Introduction In 1996 the World Health Organization declared intimate partner violence (IPV) the most important public health problem. Meta-analyses in 2013 showed every third female globally had been a victim of violence. Experts find screening controversial; family medicine is the preferred environment for identifying victims of violence, but barriers on both sides prevent patients from discussing it with doctors. Methods In July 2014, a qualitative study was performed through semi-structured interviews with ten family doctors of different ages and gender, working in rural or urban environments. Sound recordings of the interviews were transcribed, and the record verified. The data were interpreted using content analysis. A coding scheme was developed and later verified and analysed by two independent researchers. The text of the interviews was analysed according to the coding scheme. Results Two coding schemes were developed: one for screening, and the other for the active detection of IPV. The main themes emerging as barriers to screening were lack of time, staff turnover, inadequate finance, ignorance of a clear definition, poor commitment to screening, obligatory follow-up, risk of deterioration of the doctor-patient relationship, and insincerity on the part of the patient. Additionally, cultural aspects of violence, uncertainty/ helplessness, fear, lack of competence and qualifications, autonomy/negative experience, and passive role/stigma/ fear on the part of the patients were barriers to active detection. Conclusion All the participating doctors had had previous experience with active detection of IPV and were aware of its importance. Due to several barriers to screening for violence they preferred active detection.

  18. Identification of Pregnane X Receptor Ligands Using Time-Resolved Fluorescence Resonance Energy Transfer and Quantitative High-Throughput Screening

    PubMed Central

    Shukla, Sunita J.; Nguyen, Dac-Trung; MacArthur, Ryan; Simeonov, Anton; Frazee, William J.; Hallis, Tina M.; Marks, Bryan D.; Singh, Upinder; Eliason, Hildegard C.; Printen, John; Austin, Christopher P.; Inglese, James

    2009-01-01

    Abstract The human pregnane X nuclear receptor (PXR) is a xenobiotic-regulated receptor that is activated by a range of diverse chemicals, including antibiotics, antifungals, glucocorticoids, and herbal extracts. PXR has been characterized as an important receptor in the metabolism of xenobiotics due to induction of cytochrome P450 isozymes and activation by a large number of prescribed medications. Developing methodologies that can efficiently detect PXR ligands will be clinically beneficial to avoid potential drug–drug interactions. To facilitate the identification of PXR ligands, a time-resolved fluorescence resonance energy transfer (TR-FRET) assay was miniaturized to a 1,536-well microtiter plate format to employ quantitative high-throughput screening (qHTS). The optimized 1,536-well TR-FRET assay showed Z′-factors of ≥0.5. Seven- to 15-point concentration–response curves (CRCs) were generated for 8,280 compounds using both terbium and fluorescein emission data, resulting in the generation of 241,664 data points. The qHTS method allowed us to retrospectively examine single concentration screening datasets to assess the sensitivity and selectivity of the PXR assay at different compound screening concentrations. Furthermore, nonspecific assay artifacts such as concentration-based quenching of the terbium signal and compound fluorescence were identified through the examination of CRCs for specific emission channels. The CRC information was also used to define chemotypes associated with PXR ligands. This study demonstrates the feasibility of profiling thousands of compounds against PXR using the TR-FRET assay in a high-throughput format. PMID:19505231

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

    Technology Transfer Automated Retrieval System (TEKTRAN)

    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...

  20. UTILITY OF ACTIVITY AND OBSERVATIONAL DATA FOR NEUROTOXICITY SCREENING

    EPA Science Inventory

    Observational and activity tests provide neurobehavioral data critical for assessing a chemical's effects on the nervous system. he measures are sensitive, relatively specific, and provide information about the effects of the chemical in specified functional domains. These measur...

  1. Sunspot Time Series: Passive and Active Intervals

    NASA Astrophysics Data System (ADS)

    Zięba, S.; Nieckarz, Z.

    2014-07-01

    Solar activity slowly and irregularly decreases from the first spotless day (FSD) in the declining phase of the old sunspot cycle and systematically, but also in an irregular way, increases to the new cycle maximum after the last spotless day (LSD). The time interval between the first and the last spotless day can be called the passive interval (PI), while the time interval from the last spotless day to the first one after the new cycle maximum is the related active interval (AI). Minima of solar cycles are inside PIs, while maxima are inside AIs. In this article, we study the properties of passive and active intervals to determine the relation between them. We have found that some properties of PIs, and related AIs, differ significantly between two group of solar cycles; this has allowed us to classify Cycles 8 - 15 as passive cycles, and Cycles 17 - 23 as active ones. We conclude that the solar activity in the PI declining phase (a descending phase of the previous cycle) determines the strength of the approaching maximum in the case of active cycles, while the activity of the PI rising phase (a phase of the ongoing cycle early growth) determines the strength of passive cycles. This can have implications for solar dynamo models. Our approach indicates the important role of solar activity during the declining and the rising phases of the solar-cycle minimum.

  2. Not just couch potatoes or gym rats: alternative non-labor market time use patterns are associated with meeting physical activity guidelines among sedentary full-time employees

    PubMed Central

    Smith, Lindsey P.; Ng, Shu Wen; Popkin, Barry M.

    2014-01-01

    Physical activity and inactivity have distinct cardio-metabolic consequences, suggesting that combinations of activities can impact health above and beyond the effects of a single activity. However, little work has examined patterns of non-labor market time activity in the US population, particularly among full-time employees in sedentary occupations, who are at increased risk of adverse health consequences associated with a sedentary lifestyle. Identification of these patterns, and how they are related to total physical activity levels, is important for developing effective, attainable physical activity recommendations among sedentary employees, who typically have less time available for exercise. This is, especially the case for low-income employees who face the highest time and financial barriers to achieving physical activity goals. This study uses cluster analysis to examine patterns of non-labor market time use among full-time (≥40 h/week) employed adults in sedentary occupations (<3 MET-h) on working days in the American Time Use Study. We then examine whether these patterns are associated with higher likelihood of meeting physical activity recommendations and higher overall physical activity (MET-h). We find that non-labor market time use patterns include those characterized by screen activities, housework, caregiving, sedentary leisure, and exercise. For both genders, the screen pattern was the most common and increased from 2003 to 2012, while the exercise pattern was infrequent and consistent across time. Screen, sedentary leisure, and community patterns were associated with lower likelihoods of meeting physical activity recommendations, suggesting that interventions targeting screen time may miss opportunities to improve physical activity among similarly sedentary groups. Alternately, non-labor market time use patterns characterized by housework and caregiving, represented feasible avenues for increasing overall physical activity levels, especially

  3. Preference as a Function of Active Interresponse Times: A Test of the Active Time Model

    ERIC Educational Resources Information Center

    Misak, Paul; Cleaveland, J. Mark

    2011-01-01

    In this article, we describe a test of the active time model for concurrent variable interval (VI) choice. The active time model (ATM) suggests that the time since the most recent response is one of the variables controlling choice in concurrent VI VI schedules of reinforcement. In our experiment, pigeons were trained in a multiple concurrent…

  4. Association of screen time with self-perceived attention problems and hyperactivity levels in French students: a cross-sectional study

    PubMed Central

    Guichard, Elie; Kurth, Tobias

    2016-01-01

    Objective To investigate whether high levels of screen time exposure are associated with self-perceived levels of attention problems and hyperactivity in higher education students. Design Cross-sectional study among participants of the i-Share cohort. Setting French-speaking students of universities and higher education institutions. Participants 4816 graduate students who were at least 18 years old. Exposure Screen time was assessed by self-report of the average time spent on five different screen activities on smartphone, television, computer and tablet and categorised into quartiles. Main outcome measure We used the Attention Deficit Hyperactivity Disorder Self-Report Scale (ASRS-v1.1) concerning students’ behaviour over the past 6 months to measure self-perceived levels of attention problems and hyperactivity. Responses were summarised into a global score as well as scores for attention problems and hyperactivity. Results The 4816 participants of this study had a mean age of 20.8 years and 75.5% were female. Multivariable ordinary regression models showed significant associations of screen time exposure with quintiles of the total score of self-perceived attention problems and hyperactivity levels as well as the individual domains. Compared to the lowest screen time exposure category, the ORs (95% CI) were 1.58 (1.37 to 1.82) for each increasing level of quintiles of the global score, 1.57 (1.36 to 1.81) for increasing quintiles of attention levels and 1.25 (1.09 to 1.44) for increasing quartiles of hyperactivity. Conclusions Results of this large cross-sectional study among French university and higher education students show dose-dependent associations between screen time and self-perceived levels of attention problems and hyperactivity. Further studies are warranted to evaluate whether interventions could positively influence these associations. PMID:26920440

  5. Constraint factor graph cut–based active contour method for automated cellular image segmentation in RNAi screening

    PubMed Central

    CHEN, C.; LI, H.; ZHOU, X.; WONG, S. T. C.

    2010-01-01

    Summary Image-based, high throughput genome-wide RNA interference (RNAi) experiments are increasingly carried out to facilitate the understanding of gene functions in intricate biological processes. Automated screening of such experiments generates a large number of images with great variations in image quality, which makes manual analysis unreasonably time-consuming. Therefore, effective techniques for automatic image analysis are urgently needed, in which segmentation is one of the most important steps. This paper proposes a fully automatic method for cells segmentation in genome-wide RNAi screening images. The method consists of two steps: nuclei and cytoplasm segmentation. Nuclei are extracted and labelled to initialize cytoplasm segmentation. Since the quality of RNAi image is rather poor, a novel scale-adaptive steerable filter is designed to enhance the image in order to extract long and thin protrusions on the spiky cells. Then, constraint factor GCBAC method and morphological algorithms are combined to be an integrated method to segment tight clustered cells. Compared with the results obtained by using seeded watershed and the ground truth, that is, manual labelling results by experts in RNAi screening data, our method achieves higher accuracy. Compared with active contour methods, our method consumes much less time. The positive results indicate that the proposed method can be applied in automatic image analysis of multi-channel image screening data. PMID:18445146

  6. Real-Time Monitoring of Cellular Bioenergetics with a Multi-Analyte Screen-Printed Electrode

    PubMed Central

    McKenzie, Jennifer R.; Cognata, Andrew C.; Davis, Anna N.; Wikswo, John P.; Cliffel, David E.

    2016-01-01

    Real-time monitoring of changes to cellular bioenergetics can provide new insights into mechanisms of action for disease and toxicity. This work describes the development of a multi-analyte screen-printed electrode for the detection of analytes central to cellular bioenergetics: glucose, lactate, oxygen, and pH. Platinum screen-printed electrodes were designed in-house and printed by Pine Research Instrumentation. Electrochemical plating techniques were used to form quasi-reference and pH electrodes. A Dimatix materials inkjet printer was used to deposit enzyme and polymer films to form sensors for glucose, lactate, and oxygen. These sensors were evaluated in bulk solution and microfluidic environments, and found to behave reproducibly and possess a lifetime of up to six weeks. Linear ranges and limits of detection for enzyme-based sensors were found to have an inverse relationship with enzyme loading, and iridium oxide pH sensors were found to have super-Nernstian responses. Preliminary measurements where the sensor was enclosed within a microfluidic channel with RAW 264.7 macrophages were performed to demonstrate the sensors’ capabilities for performing real-time microphysiometry measurements. PMID:26125545

  7. No Time To Lose - High Throughput Screening To Assess Nanomaterial Safety

    PubMed Central

    Damoiseaux, R; George, S; Li, M; Pokhrel, S; Ji, Z; France, B; Xia, T; Suarez, E; Rallo, R; Mädler, L; Cohen, Y; Hoek, EMV; Nel, A

    2014-01-01

    Nanomaterials hold great promise for medical, technological and economical benefits. Knowledge concerning the toxicological properties of these novel materials is typically lacking. At the same time, it is becoming evident that some nanomaterials could have a toxic potential in humans and the environment. Animal based systems lack the needed capacity to cope with the abundance of novel nanomaterials being produced, and thus we have to employ in vitro methods with high throughput to manage the rush logistically and use high content readouts wherever needed in order to gain more depth of information. Towards this end, high throughput screening (HTS) and high content screening (HCS) approaches can be used to speed up the safety analysis on a scale that commensurate with the rate of expansion of new materials and new properties. The insights gained from HTS/HCS should aid in our understanding of the tenets of nanomaterial hazard at biological level as well as asset the development of safe-by-design approaches. This review aims to provide a comprehensive introduction to the HTS/HCS methodology employed for safety assessment of engineered nanomaterials (ENMs), including data analysis and prediction of potentially hazardous material properties. Given the current pace of nanomaterial development, HTS/HCS is a potentially effective means of keeping up with the rapid progress in this field – we have literally no time to lose. PMID:21301704

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

    PubMed

    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. PMID:25154878

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

    PubMed Central

    Astani, Akram; Reichling, Jürgen; Schnitzler, Paul

    2011-01-01

    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. PMID:20008902

  10. Screening for antiviral activities of isolated compounds from essential oils.

    PubMed

    Astani, Akram; Reichling, Jürgen; Schnitzler, Paul

    2011-01-01

    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. PMID:20008902

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

    PubMed

    Hamada, Nagwa Mohamed Mahrous; Abdo, Nadia Yousef Megally

    2015-01-01

    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. PMID:26060913

  12. Endocrine disruptors in bottled mineral water: estrogenic activity in the E-Screen.

    PubMed

    Wagner, Martin; Oehlmann, Jörg

    2011-10-01

    Human exposure to endocrine disruptors is well documented by biomonitoring data. However, this information is limited to few chemicals like bisphenol A or phthalate plasticizers. To account for so-far unidentified endocrine disruptors and potential mixture effects we employ bioassays to detect endocrine activity in foodstuff and consequently characterize the integrated exposure to endocrine active compounds. Recently, we reported a broad contamination of commercially available bottled water with estrogenic activity and presented evidence for the plastic packaging being a source of this contamination. In continuation of that work, we here compare different sample preparation methods to extract estrogen-like compounds from bottled water. These data demonstrate that inappropriate extraction methods and sample treatment may lead to false-negative results when testing water extracts in bioassays. Using an optimized sample preparation strategy, we furthermore present data on the estrogenic activity of bottled water from France, Germany, and Italy: eleven of the 18 analyzed water samples (61.1%) induced a significant estrogenic response in a bioassay employing a human carcinoma cell line (MCF7, E-Screen). The relative proliferative effects ranged from 19.8 to 50.2% corresponding to an estrogenic activity of 1.9-12.2 pg estradiol equivalents per liter bottled water. When comparing water of the same spring that is packed in glass or plastic bottles made of polyethylene terephthalate (PET), estrogenic activity is three times higher in water from plastic bottles. These data support the hypothesis that PET packaging materials are a source of estrogen-like compounds. Furthermore, the findings presented here conform to previous studies and indicate that the contamination of bottled water with endocrine disruptors is a transnational phenomenon. PMID:21050888

  13. Seasonal variation in leisure time physical activity.

    PubMed

    Uitenbroek, D G

    1993-06-01

    In this paper seasonal variation in leisure time physical activity for exercise is studied and quantified with regard to several popular exercise activities and taking the respondents gender, occupational status, and age into consideration. The analysis concerns data collected by telephone in Scotland between January 1989 and March 1992. Data from 7,202 male and 9,284 female respondents is used in the analysis; cosinor analysis using GLIM is applied. Considerable seasonal variation was found affecting both outdoor and indoor activities. During the peak phase in July, 32% of the respondents reported exercising for at least 20 min three or more times during the previous week, in the winter period this decreased to 23%. Older respondents were found to exercise more later in the year and also showed seasonal variation to a larger extent than younger respondents. This is particularly so for those respondents who exercise at a relatively high frequency. PMID:8321115

  14. The non-advertising effects of screen-based sedentary activities on acute eating behaviours in children, adolescents, and young adults. A systematic review.

    PubMed

    Marsh, Samantha; Ni Mhurchu, Cliona; Maddison, Ralph

    2013-12-01

    Sedentary screen time may be an important determinant of childhood obesity. A number of potential mechanisms to explain the link between screen time and increased bodyweight have been proposed; however, the relationship appears to be best explained by the effects on dietary intake, which is attributed to either food advertising or effects independent of food advertising. Technological advances have allowed for greater accessibility and exposure to advertisement-free screen-based media. This review was conducted to systematically synthesise the evidence from laboratory based studies which have investigated the non-advertising effects of screen time (TV viewing, sedentary video games, and computer use) on dietary intake in children, adolescents, and young adults. MEDLINE, PubMed, PsychInfo, CINAHL, and Embase were searched from inception through 5 July 2013. Ten trials met the inclusion criteria and were included in the review. Risk of study bias was judged to range from low to high. Screen time in the absence of food advertising was consistently found to be associated with increased dietary intake compared with non-screen behaviours. Suggested explanations for this relationship included: distraction, interruption of physiologic food regulation, screen time as a conditioned cue to eat, disruption of memory formation, and the effects of the stress-induced reward system. Due to the limited number of high-quality studies available for this review, our findings are preliminary. More work is required to better establish the link between dietary intake and advertisement-free screen time and assess whether differences exist between the different screen-based activities. PMID:24001394

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

    PubMed

    Pickford, Daniel B

    2010-11-01

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

  16. Cytotoxic activity screening of Bangladeshi medicinal plant extracts.

    PubMed

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

    2014-01-01

    The cytotoxic activity of 23 crude methanol extracts from 19 Bangladeshi medicinal plants was investigated against healthy mouse fibroblasts (NIH3T3), healthy monkey kidney (VERO) and four human cancer cell lines (gastric, AGS; colon, HT-29; and breast, MCF-7 and MDA-MB-231) using MTT assay. High cytotoxicity across all cell lines tested was exhibited by Aegiceras corniculatum (fruit) and Hymenodictyon excelsum (bark) extracts (IC50 values ranging from 0.0005 to 0.9980 and 0.08 to 0.44 mg/mL, respectively). Fourteen extracts from 11 plant species, namely Clitoria ternatea (flower and leaf), Dillenia indica (leaf), Diospyros peregrina (leaf), Dipterocarpus turbinatus (bark and leaf), Ecbolium viride (leaf), Glinus oppositifolius (whole plant), Gnaphalium luteoalbum (leaf), Jasminum sambac (leaf), Lannea coromandelica (bark and leaf), Mussaenda glabrata (leaf) and Saraca asoca (leaf), were also significantly cytotoxic (IC50 < 1.0 mg/mL) against at least one of the cancer cell lines tested. More selectively, Avicennia alba (leaf), C. ternatea (flower and leaf), Caesalpinia pulcherrima (leaf), E. viride (leaf) and G. oppositifolius (whole plant) showed cytotoxicity only against both of the breast cancer cell lines (MCF-7 and MDA-MB-231). In contrast, C. ternatea (flower and leaf) exhibited high cytotoxic activity against MDA-MB-231 (IC50 values of 0.11 and 0.49 mg/mL, respectively), whereas E. viride and G. oppositifolius whole plant extracts exhibited high activity against MCF-7 cells (IC50 values of 0.06 and 0.15 mg/mL, respectively). The cytotoxic activity test results for 9 of the plant species correlate with their traditional use as anticancer agents, thus making them interesting sources for further drug development. PMID:23846168

  17. Screening for fractions of Oxytropis falcata Bunge with antibacterial activity.

    PubMed

    Jiang, H; Hu, J R; Zhan, W Q; Liu, X

    2009-01-01

    Preliminary studies with the four extracts of Oxytropis falcate Bunge exhibited that the chloroform and ethyl acetate extracts showed stronger antibacterial activities against the nine tested Gram-positive and Gram-negative bacteria. The HPLC-scanned and bioassay-guided fractionation led to the isolation and identification of the main flavonoid compounds, i.e. rhamnocitrin, kaempferol, rhamnetin, 2',4'-dihydroxychalcone and 2',4',beta-trihydroxy-dihydrochalcon. Except 2',4',beta-trihydroxy-dihydrochalcon, four other compounds had good antibacterial activities. The minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) of the four compounds ranged between 125 and 515 microg mL(-1). Staphylococcus aureus was the most susceptible to these compounds, with MIC and MBC values from 125 to 130 microg mL(-1). This is the first report of antibacterial activity in O. falcate Bunge. In this study, evidence to evaluate the biological functions of O. falcate Bunge is provided, which promote the rational use of this herb. PMID:19521909

  18. Preclinical screening of phyllanthus amarus ethanolic extract for its analgesic and antimicrobial activity

    PubMed Central

    Bhat, S. Sham; Hegde, K. Sundeep; Chandrashekhar, Sharath; Rao, S. N.; Manikkoth, Shyamjith

    2015-01-01

    Background: To discover a new agent which possesses dual property of analgesic and antimicrobial activity, thereby reducing the burden of polypharmacy. Phyllanthus amarus was screened for its analgesic and antimicrobial activities. Objectives: The objective was to evaluate the analgesic and antimicrobial activity, of P. amarus ethanolic extract (PAEE). Materials and Methods: The ethanolic extract of P. amarus was prepared using Soxhlet apparatus. An in vivo study using Swiss albino mice was done to screen the central and peripheral analgesic activity of P. amarus extract. The extract was administered at a dose of 100 mg/kg body weight orally. The peripheral analgesic activity was assessed using acetic acid induced writhing test. The central analgesic activity was assessed using Eddy's hot plate apparatus. An in vitro study was carried out to study the antimicrobial activity of the above extract using selected species of Streptococcus mutans, and S. salivarius. The antimicrobial activities were determined using the agar well method. Results: The ethanolic extract of P. amarus showed significant (P < 0.05) peripheral and central analgesic activity. In vitro antimicrobial screening indicated that the ethanolic extract had shown a zone of inhibition against S. mutans and S. salivarius in the agar wells. Conclusion: This study showed that PAEE exhibited significant analgesic and antimicrobial activities. PMID:26692753

  19. A novel cell-based duplex high-throughput screening assay combining fluorescent Ca(2+) measurement with homogeneous time-resolved fluorescence technology.

    PubMed

    Kiss, László; Cselenyák, Attila; Varga, Ágnes; Visegrády, András

    2016-08-15

    Cell-based assays for G-protein-coupled receptor (GPCR) activation applied in high-throughput screening (HTS) monitor various readouts for second messengers or intracellular effectors. Recently, our understanding of diverging signaling pathways downstream of receptor activation and the capability of small molecules to selectively modulate signaling routes has increased substantially, underlining the importance of selecting appropriate readouts in cellular functional screens. To minimize the rate of false negatives in large-scale screening campaigns, it is crucial to maximize the chance of a ligand being detected, and generally applicable methods for detecting multiple analytes from a single well might serve this purpose. The few assays developed so far based on multiplexed GPCR readouts are limited to only certain applications and usually rely on genetic manipulations hindering screening in native or native-like cellular systems. Here we describe a more generally applicable and HTS-compatible homogeneous assay based on the combination of fluorometric detection of [Ca(2+)] with subsequent homogeneous time-resolved fluorescence (HTRF) cAMP readout in the same well. Besides describing development and validation of the assay, using a cell line recombinantly expressing the human PTH1 receptor screening of a small library is also presented, demonstrating the robustness and HTS compatibility of the novel paradigm. PMID:27235172

  20. A screening for antimicrobial activities of Caribbean herbal remedies

    PubMed Central

    2013-01-01

    Background The TRAMIL program aims to understand, validate and expand health practices based on the use of medicinal plants in the Caribbean, which is a “biodiversity hotspot” due to high species endemism, intense development pressure and habitat loss. The antibacterial activity was examined for thirteen plant species from several genera that were identified as a result of TRAMIL ethnopharmacological surveys or were reported in ethnobotanical accounts from Puerto Rico. The aim of this study was to validate the traditional use of these plant species for the treatment of bacterial infections, such as conjunctivitis, fever, otitis media and furuncles. Methods An agar disc diffusion assay was used to examine five bacterial strains that are associated with the reported infections, including Staphylococcus saprophyticus (ATCC 15305), S. aureus (ATCC 6341), Escherichia coli (ATCC 4157), Haemophilus influenzae (ATCC 8142), Pseudomonas aeruginosa (ATCC 7700) and Proteus vulgaris (ATCC 6896), as well as the fungus Candida albicans (ATCC 752). The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values were determined for each of the extracts that showed inhibitory activity. Results The decoctions of Pityrogramma calomelanos, Tapeinochilus ananassae, and Syzygium jambos, as well as the juice of Gossypium barbadense, showed > 20% growth inhibition against several bacteria relative to the positive control, which was the antibiotic Streptomycin. Extracts with the best antimicrobial activities were S. jambos that showed MIC = 31 μg/mL and MBC = 1.0 mg/mL against P. vulgaris and T. ananassae that showed MIC = 15 μg/mL against S. aureus. Conclusion This report confirms the traditional use of P. calomelanos for the treatment of kidney infections that are associated with stones, as well as the antimicrobial and bactericidal effects of T. ananassae against P. vulgaris and S. saprophyticus and the effects of S. jambos against S

  1. Screening of Panamanian Plant Extracts for Pesticidal Properties and HPLC-Based Identification of Active Compounds

    PubMed Central

    Guldbrandsen, Niels; De Mieri, Maria; Gupta, Mahabir; Seiser, Tobias; Wiebe, Christine; Dickhaut, Joachim; Reingruber, Rüdiger; Sorgenfrei, Oliver; Hamburger, Matthias

    2015-01-01

    A library of 600 taxonomically diverse Panamanian plant extracts was screened for fungicidal, insecticidal, and herbicidal activities. A total of 19 active extracts were submitted to HPLC-based activity profiling, and extracts of Bocconia frutescens, Miconia affinis, Myrcia splendens, Combretum aff. laxum, and Erythroxylum macrophyllum were selected for the isolation of compounds. Chelerythrine (2), macarpine (3), dihydrosanguinarine (5), and arjunolic acid (8) showed moderate-to-good fungicidal activity. Myricetin-3-O-(6’’-O-galloyl)-β-galactopyranoside (13) showed moderate insecticidal activity, but no compound with herbicidal activity was identified. PMID:26839818

  2. Time of flight secondary ion mass spectrometry: A powerful high throughput screening tool

    NASA Astrophysics Data System (ADS)

    Smentkowski, Vincent S.; Ostrowski, Sara G.

    2007-07-01

    Combinatorial materials libraries are becoming more complicated; successful screening of these libraries requires the development of new high throughput screening methodologies. Time of flight secondary ion mass spectrometry (ToF-SIMS) is a surface analytical technique that is able to detect and image all elements (including hydrogen which is problematic for many other analysis instruments) and molecular fragments, with high mass resolution, during a single measurement. Commercial ToF-SIMS instruments can image 500μm areas by rastering the primary ion beam over the region of interest. In this work, we will show that large area analysis can be performed, in one single measurement, by rastering the sample under the ion beam. We show that an entire 70mm diameter wafer can be imaged in less than 90min using ToF-SIMS stage (macro)rastering techniques. ToF-SIMS data sets contain a wealth of information since an entire high mass resolution mass spectrum is saved at each pixel in an ion image. Multivariate statistical analysis (MVSA) tools are being used in the ToF-SIMS community to assist with data interpretation; we will demonstrate that MVSA tools provide details that were not obtained using manual (univariate) analysis.

  3. Antepartum Screening for Maternal Infection and Immune Status: Is it Time to Broaden Our Routine?

    PubMed

    Poliquin, Vanessa; Yudin, Mark H; Murphy, Kellie E; Okun, Nan

    2015-12-01

    Maternal infections with PVB19, HCV, CMV, and HIV during the antepartum period are important health problems for which the technological capacities for screening and diagnosis during the antepartum period are available. Each of these viruses requires individual consideration for inclusion in screening and for the method of screening during the antepartum period. The availability of efficacious treatments for HCV and CMV, with demonstrable benefits to the mother or fetus, is required before antepartum screening for these infections can be justified. Screening for parvovirus B19 presents a greater concern because it meets most of the features of a screening test (Wilson’s criteria) endorsed by the WHO. There is insufficient evidence to argue strongly for implementation of antepartum PVB19 screening, but the available evidence indicates a need for large studies of potential effectiveness and costs of routine PVB19 screening, either for all pregnant woman or for those at high risk of exposure to PVB19. While the technology to screen for HCV, PVB19, and CMV certainly exists, there must be careful consideration of the downstream implications of routine screening at the level of the individual patient, the general population, and other health care resources, including laboratory infrastructure, before recommending that these infections be screened for routinely in the antepartum period. A strategy for national adoption of an opt-out screening strategy for HIV should be considered. PMID:26637086

  4. High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni.

    PubMed

    Mansour, Nuha R; Paveley, Ross; Gardner, J Mark F; Bell, Andrew S; Parkinson, Tanya; Bickle, Quentin

    2016-04-01

    An estimated 600 million people are affected by the helminth disease schistosomiasis caused by parasites of the genus Schistosoma. There is currently only one drug recommended for treating schistosomiasis, praziquantel (PZQ), which is effective against adult worms but not against the juvenile stage. In an attempt to identify improved drugs for treating the disease, we have carried out high throughput screening of a number of small molecule libraries with the aim of identifying lead compounds with balanced activity against all life stages of Schistosoma. A total of almost 300,000 compounds were screened using a high throughput assay based on motility of worm larvae and image analysis of assay plates. Hits were screened against juvenile and adult worms to identify broadly active compounds and against a mammalian cell line to assess cytotoxicity. A number of compounds were identified as promising leads for further chemical optimization. PMID:27128493

  5. High Throughput Screening Identifies Novel Lead Compounds with Activity against Larval, Juvenile and Adult Schistosoma mansoni

    PubMed Central

    Gardner, J. Mark F.; Bell, Andrew S.; Parkinson, Tanya; Bickle, Quentin

    2016-01-01

    An estimated 600 million people are affected by the helminth disease schistosomiasis caused by parasites of the genus Schistosoma. There is currently only one drug recommended for treating schistosomiasis, praziquantel (PZQ), which is effective against adult worms but not against the juvenile stage. In an attempt to identify improved drugs for treating the disease, we have carried out high throughput screening of a number of small molecule libraries with the aim of identifying lead compounds with balanced activity against all life stages of Schistosoma. A total of almost 300,000 compounds were screened using a high throughput assay based on motility of worm larvae and image analysis of assay plates. Hits were screened against juvenile and adult worms to identify broadly active compounds and against a mammalian cell line to assess cytotoxicity. A number of compounds were identified as promising leads for further chemical optimization. PMID:27128493

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

    PubMed

    Huang, Ruili

    2016-01-01

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

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

    PubMed Central

    Puig-Ribera, Anna; Martín-Cantera, Carlos; Puigdomenech, Elisa; Real, Jordi; Romaguera, Montserrat; Magdalena-Belio, José Félix; Recio-Rodríguez, Jose Ignacio; Rodriguez-Martin, Beatriz; Arietaleanizbeaskoa, Maria Soledad; Repiso–Gento, Irene; Garcia-Ortiz, Luis

    2015-01-01

    Objectives 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). Methods 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. Results 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

  8. Screen Time, How Much Is Too Much? The Social and Emotional Costs of Technology on the Adolescent Brain

    ERIC Educational Resources Information Center

    DeWeese, Katherine Lynn

    2014-01-01

    Screen time no longer means just the amount of time one spends in front of the television. Now it is an aggregate amount of time spent on smartphones, computers as well as multitasking with different devices. How much are the glowing rectangles taking away from adolescent social and emotional health? How is it changing how students learn and how…

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

    PubMed

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

    2016-12-15

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

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

    PubMed

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

    2016-01-01

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

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

    PubMed Central

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

    2016-01-01

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

  12. Ethnobotanical study, antifungal activity, phytochemical screening and total phenolic content of Algerian Aristolochia longa

    PubMed Central

    Benarba, Bachir; Meddah, Boumedienne

    2014-01-01

    Aim: Aristolochia longa (from the family Aristolochiaceae) is widely used in Algerian traditional medicine. Here, we document ethnomedicinal uses by local population of Mascara province (West Algeria) and we evaluate the antifungal activity, the phytochemical composition and total phenolic content of aqueous extract (decoction) of the roots of A. longa from Algeria. Materials and Methods: The ethnobotanical investigation was carried out in Mascara Province (West Algeria). Antifungal activity was assessed against Saccharomyces cerevisiae. Total phenolic content was measured using the Folin–Ciocalteu’s reagent. Results: Our results showed that A. longa is widely used to treat several ailments such as cancer (38%), skin infections (14%), and diabetes (11%). Crushed roots are commonly used (89%) mixed with honey, milk, water or other medicinal plants. A. longa aqueous extract induced growth inhibition of S. cerevisiae cells in a dose - and time - dependent manner. An effective suppression of S. cerevisiae (97.06% inhibition of proliferation) was obtained at the 500 µg/mL after 72 h. Results of the phytochemical screening revealed that A. longa aqueous extract contained various bioactive compounds, including polyphenols and flavonoids. Total phenolic content in A. longa aqueous extract was found to be 6.07 ± 0.12 mg (gallic acid equivalents)/g. Conclusion: A. longa may be considered as a promising source of new drugs for treating cancer and as a good antifungal agent. PMID:26401365

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

    PubMed Central

    Selin, Carrie; Stietz, Maria S.; Blanchard, Jan E.; Hall, Dennis G.; Brown, Eric D.; Cardona, Silvia T.

    2015-01-01

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

  14. 78 FR 38452 - Agency Information Collection (VA Police Officer Pre-Employment Screening Checklist) Activities...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-06-26

    ... AFFAIRS Agency Information Collection (VA Police Officer Pre-Employment Screening Checklist) Activities... ``OMB Control No. 2900-0524.'' SUPPLEMENTARY INFORMATION: Title: VA Police Officer Pre-Employment... checks on applicants seeking employment as VA police officers. VA will use the data collected...

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

    PubMed

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

    2015-01-01

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

  16. Screen media usage, sleep time and academic performance in adolescents: clustering a self-organizing maps analysis.

    PubMed

    Peiró-Velert, Carmen; Valencia-Peris, Alexandra; González, Luis M; García-Massó, Xavier; Serra-Añó, Pilar; Devís-Devís, José

    2014-01-01

    Screen media usage, sleep time and socio-demographic features are related to adolescents' academic performance, but interrelations are little explored. This paper describes these interrelations and behavioral profiles clustered in low and high academic performance. A nationally representative sample of 3,095 Spanish adolescents, aged 12 to 18, was surveyed on 15 variables linked to the purpose of the study. A Self-Organizing Maps analysis established non-linear interrelationships among these variables and identified behavior patterns in subsequent cluster analyses. Topological interrelationships established from the 15 emerging maps indicated that boys used more passive videogames and computers for playing than girls, who tended to use mobile phones to communicate with others. Adolescents with the highest academic performance were the youngest. They slept more and spent less time using sedentary screen media when compared to those with the lowest performance, and they also showed topological relationships with higher socioeconomic status adolescents. Cluster 1 grouped boys who spent more than 5.5 hours daily using sedentary screen media. Their academic performance was low and they slept an average of 8 hours daily. Cluster 2 gathered girls with an excellent academic performance, who slept nearly 9 hours per day, and devoted less time daily to sedentary screen media. Academic performance was directly related to sleep time and socioeconomic status, but inversely related to overall sedentary screen media usage. Profiles from the two clusters were strongly differentiated by gender, age, sedentary screen media usage, sleep time and academic achievement. Girls with the highest academic results had a medium socioeconomic status in Cluster 2. Findings may contribute to establishing recommendations about the timing and duration of screen media usage in adolescents and appropriate sleep time needed to successfully meet the demands of school academics and to improve

  17. Screen Media Usage, Sleep Time and Academic Performance in Adolescents: Clustering a Self-Organizing Maps Analysis

    PubMed Central

    Peiró-Velert, Carmen; Valencia-Peris, Alexandra; González, Luis M.; García-Massó, Xavier; Serra-Añó, Pilar; Devís-Devís, José

    2014-01-01

    Screen media usage, sleep time and socio-demographic features are related to adolescents' academic performance, but interrelations are little explored. This paper describes these interrelations and behavioral profiles clustered in low and high academic performance. A nationally representative sample of 3,095 Spanish adolescents, aged 12 to 18, was surveyed on 15 variables linked to the purpose of the study. A Self-Organizing Maps analysis established non-linear interrelationships among these variables and identified behavior patterns in subsequent cluster analyses. Topological interrelationships established from the 15 emerging maps indicated that boys used more passive videogames and computers for playing than girls, who tended to use mobile phones to communicate with others. Adolescents with the highest academic performance were the youngest. They slept more and spent less time using sedentary screen media when compared to those with the lowest performance, and they also showed topological relationships with higher socioeconomic status adolescents. Cluster 1 grouped boys who spent more than 5.5 hours daily using sedentary screen media. Their academic performance was low and they slept an average of 8 hours daily. Cluster 2 gathered girls with an excellent academic performance, who slept nearly 9 hours per day, and devoted less time daily to sedentary screen media. Academic performance was directly related to sleep time and socioeconomic status, but inversely related to overall sedentary screen media usage. Profiles from the two clusters were strongly differentiated by gender, age, sedentary screen media usage, sleep time and academic achievement. Girls with the highest academic results had a medium socioeconomic status in Cluster 2. Findings may contribute to establishing recommendations about the timing and duration of screen media usage in adolescents and appropriate sleep time needed to successfully meet the demands of school academics and to improve

  18. A Portable Real-Time Ringdown Breath Acetone Analyzer: Toward Potential Diabetic Screening and Management.

    PubMed

    Jiang, Chenyu; Sun, Meixiu; Wang, Zhennan; Chen, Zhuying; Zhao, Xiaomeng; Yuan, Yuan; Li, Yingxin; Wang, Chuji

    2016-01-01

    Breath analysis has been considered a suitable tool to evaluate diseases of the respiratory system and those that involve metabolic changes, such as diabetes. Breath acetone has long been known as a biomarker for diabetes. However, the results from published data by far have been inconclusive regarding whether breath acetone is a reliable index of diabetic screening. Large variations exist among the results of different studies because there has been no "best-practice method" for breath-acetone measurements as a result of technical problems of sampling and analysis. In this mini-review, we update the current status of our development of a laser-based breath acetone analyzer toward real-time, one-line diabetic screening and a point-of-care instrument for diabetic management. An integrated standalone breath acetone analyzer based on the cavity ringdown spectroscopy technique has been developed. The instrument was validated by using the certificated gas chromatography-mass spectrometry. The linear fittings suggest that the obtained acetone concentrations via both methods are consistent. Breath samples from each individual subject under various conditions in total, 1257 breath samples were taken from 22 Type 1 diabetic (T1D) patients, 312 Type 2 diabetic (T2D) patients, which is one of the largest numbers of T2D subjects ever used in a single study, and 52 non-diabetic healthy subjects. Simultaneous blood glucose (BG) levels were also tested using a standard diabetic management BG meter. The mean breath acetone concentrations were determined to be 4.9 ± 16 ppm (22 T1D), and 1.5 ± 1.3 ppm (312 T2D), which are about 4.5 and 1.4 times of the one in the 42 non-diabetic healthy subjects, 1.1 ± 0.5 ppm, respectively. A preliminary quantitative correlation (R = 0.56, p < 0.05) between the mean individual breath acetone concentration and the mean individual BG levels does exist in 20 T1D subjects with no ketoacidosis. No direct correlation is observed in T1D subjects, T2D

  19. Shackleton's Antarctic Adventure: The Greatest Survival Story of All Time. Teacher's Guide To Accompany the Giant-Screen Film.

    ERIC Educational Resources Information Center

    Gibb, Reen

    This teacher's guide was developed to accompany the giant-screen film, "Shackleton's Antarctic Adventure". The activities featured use a multidisciplinary approach and target students ages 7 through 14. Teacher pages include background information and student pages include instructions and additional information for understanding the activity.…

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

    PubMed Central

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

    2016-01-01

    This study used structurating activity theory to analyze 21 conversations between genetic counselors and individuals at increased risk for familial colorectal cancer (CRC). The qualitative analysis revealed ways elements of family, primary healthcare, cancer prevention and treatment, and other systems emerged in intervention conversations as shaping CRC screening attitudes and behaviors. Results indicate that family stories, norms, and roles are resources for enacting health practices in families and that the authority of healthcare providers is a resource for making screening decisions. Conclusions include practical implications for using findings in clinical applications as well as future research directions to build on this exploratory study. PMID:27182185

  1. PROTEOMICS IN ECOTOXICOLOGY: PROTEIN EXPRESSION PROFILING TO SCREEN CHEMICALS FOR ENDOCRINE ACTIVITY

    EPA Science Inventory

    Abstract for poster.

    Current endocrine testing methods are animal intensive and lack the throughput necessary to screen large numbers of environmental chemicals for adverse effects. In this study, Matrix Assisted Laser Desorption/Ionization Time-of-Flight Mass Spectrometry...

  2. Studies on free radical scavenging activity in Chinese seaweeds part I. Screening results

    NASA Astrophysics Data System (ADS)

    Yan, Xiao-Jun; Fang, Guo-Ming; Lou, Qing-Xiang

    1999-09-01

    Antioxidants have attracted the attention of researchers due to their beneficial effects as free radical scavengers. Application of a stable free radical named 1, 1-diphenyl-2-picrylhydrazyl(DPPH) to screen the free radical scavenging activity in 27 species of Chinese seaweed showed that 15 of them had significant activity in at least one of the organic solvent extracts. The most interesting seaweed species were Gelidium amansii, Gloiosiphonia capillaris, Polysiphonia urceolata, Sargassum kjellmanianum, Desmarestia viridis, and Rhodomela teres.

  3. Two-Step Bipolar Electrochemistry: Generation of Composition Gradient and Visual Screening of Electrocatalytic Activity.

    PubMed

    Termebaf, Hajar; Shayan, Mohsen; Kiani, Abolfazl

    2015-12-01

    Bipolar electrochemistry (BE) is employed for both creating electrocatalysts composition gradient and visual screening of the prepared composition on a single substrate in just two experiment runs. In a series of proof-of-principle experiments, we demonstrate gradient electrodeposition of Ni-Cu using BE; then the electrocatalytic activity of the prepared composition gradient toward the hydrogen evolution reaction (HER) is visually screened in the BE system using array of BPEs. Moreover, the morphology and the chemical composition of the Ni-Cu gradient are screened along the length of the bipolar electrode (BPE). By measuring the potential gradient over the BPE, it is also demonstrated that by controlling the concentration of the metals precursor and the supporting electrolyte, the length of the bipolar electrodeposited gradient can be controlled. PMID:26595192

  4. Application of the E-screen assay to test for oestrogenically active substances in swine feed.

    PubMed

    Bitsch, N; Körner, W; Postupka, S; Brunn, H

    2001-12-01

    A pig breeder in central Hesse (Germany) noticed the occurrence of enlarged vulvae in female piglets. Intoxication with oestrogenically active substances by contamination of two feed mixes ingested by the mother sows appeared to be a possible cause. Using a combined technique of the DFG analytical method S19 and the E-screen assay, two feed samples were found to contain powerful oestrogenically active compounds. By co-incubation with the anti-oestrogen tamoxifen it could be clearly demonstrated that the oestrogenic activity was mediated by the oestrogen receptor. These results demonstrate that use of the E-screen assay in combination with the DFG analytical method S19 provides a simple and readily usable prescreening method for the routine detection of oestrogenically active compounds in animal feed. The results from the E-screen assay show that the sows ingested 10-80 microg oestradiol equivalents per day in their feed. Because of the bioavailability of these substances, the oestrogenic active compounds seem to be transferred into the milk and passed to the piglets via suckling. The milk of the dam appears to contain this substance in biologically active form and at such high concentrations that the female piglets had enlarged vulvae. PMID:11906561

  5. Recreational Screen-Time Among Chinese Adolescents: A Cross-Sectional Study

    PubMed Central

    Jiang, Xiao-Xiao; Hardy, Louise L.; Ding, Ding; Baur, Louise A.; Shi, Hui-Jing

    2014-01-01

    Background Rapid urbanization in China has led to a proliferation of electronic entertainment media among youth. Prolonged screen time (ST; includes watching television and playing on computers, video game consoles, or mobile phones) is linked to poor health profiles. The aim of this study was to report recreational ST behaviors and ST correlates among Chinese adolescents living in two regions with different degrees of urbanization. Methods A cross-sectional, school-based survey (n = 3461 adolescents; aged 12–14 years old) living in inner-city Shanghai and a peri-urban region of Hangzhou. Students completed a questionnaire including family characteristics, daily ST, and information on family environment related to screen use. Recreational ST was categorized into two groups according to recommendations by the American Academy of Pediatrics (< or ≥2 h/day). Parents reported their own ST and also reported educational attainment as a proxy for socioeconomic status. Results ST was higher among boys than girls and on weekends than weekdays. Peri-urban girls were more likely to exceed 2 h/day ST compared to inner-city girls on weekends. Having a father with no university degree, mother’s TV viewing ≥2 h/day, no ST rules at home, and eating meals in front of the TV were associated with higher ST on both weekdays and weekends, and regional differences were found for weekend ST. Conclusions TV viewing and playing on the computer were the most prevalent ST behaviors among Chinese adolescents. Mobile phone playing was less prevalent but persistent throughout the week. More population-level surveillance and research is needed to monitor the trends in ST behaviors and to better understand the characteristics of those who are at risk. PMID:24930472

  6. piggyBac transposon somatic mutagenesis with an activated reporter and tracker (PB-SMART) for genetic screens in mice.

    PubMed

    Landrette, Sean F; Cornett, Jonathan C; Ni, Thomas K; Bosenberg, Marcus W; Xu, Tian

    2011-01-01

    Somatic forward genetic screens have the power to interrogate thousands of genes in a single animal. Retroviral and transposon mutagenesis systems in mice have been designed and deployed in somatic tissues for surveying hematopoietic and solid tumor formation. In the context of cancer, the ability to visually mark mutant cells would present tremendous advantages for identifying tumor formation, monitoring tumor growth over time, and tracking tumor infiltrations and metastases into wild-type tissues. Furthermore, locating mutant clones is a prerequisite for screening and analyzing most other somatic phenotypes. For this purpose, we developed a system using the piggyBac (PB) transposon for somatic mutagenesis with an activated reporter and tracker, called PB-SMART. The PB-SMART mouse genetic screening system can simultaneously induce somatic mutations and mark mutated cells using bioluminescence or fluorescence. The marking of mutant cells enable analyses that are not possible with current somatic mutagenesis systems, such as tracking cell proliferation and tumor growth, detecting tumor cell infiltrations, and reporting tissue mutagenesis levels by a simple ex vivo visual readout. We demonstrate that PB-SMART is highly mutagenic, capable of tumor induction with low copy transposons, which facilitates the mapping and identification of causative insertions. We further integrated a conditional transposase with the PB-SMART system, permitting tissue-specific mutagenesis with a single cross to any available Cre line. Targeting the germline, the system could also be used to conduct F1 screens. With these features, PB-SMART provides an integrated platform for individual investigators to harness the power of somatic mutagenesis and phenotypic screens to decipher the genetic basis of mammalian biology and disease. PMID:22039523

  7. Compound image compression for real-time computer screen image transmission.

    PubMed

    Lin, Tony; Hao, Pengwei

    2005-08-01

    We present a compound image compression algorithm for real-time applications of computer screen image transmission. It is called shape primitive extraction and coding (SPEC). Real-time image transmission requires that the compression algorithm should not only achieve high compression ratio, but also have low complexity and provide excellent visual quality. SPEC first segments a compound image into text/graphics pixels and pictorial pixels, and then compresses the text/graphics pixels with a new lossless coding algorithm and the pictorial pixels with the standard lossy JPEG, respectively. The segmentation first classifies image blocks into picture and text/graphics blocks by thresholding the number of colors of each block, then extracts shape primitives of text/graphics from picture blocks. Dynamic color palette that tracks recent text/graphics colors is used to separate small shape primitives of text/graphics from pictorial pixels. Shape primitives are also extracted from text/graphics blocks. All shape primitives from both block types are losslessly compressed by using a combined shape-based and palette-based coding algorithm. Then, the losslessly coded bitstream is fed into a LZW coder. Experimental results show that the SPEC has very low complexity and provides visually lossless quality while keeping competitive compression ratios. PMID:16121449

  8. Screening of Pharmacologically Active Small Molecule Compounds Identifies Antifungal Agents Against Candida Biofilms

    PubMed Central

    Watamoto, Takao; Egusa, Hiroshi; Sawase, Takashi; Yatani, Hirofumi

    2015-01-01

    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 Candida 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 nine 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 candidiasis. PMID

  9. Time-resolved luminescence screening method for enrofloxacin in beef serum

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Enrofloxacin is one of only two fluoroquinolone antibiotics approved for use in cattle in the U.S. Microbial screening methods currently used in the U.S. for monitoring veterinary drug residues are not sensitive or selective for fluoroquinolones. In this work, a luminescence-based screening assay ...

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

    PubMed

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

    2015-04-01

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

  11. Brief Report: Association between Socio-Demographic Factors, Screen Media Usage and Physical Activity by Type of Day in Spanish Adolescents

    ERIC Educational Resources Information Center

    Devis-Devis, Jose; Peiro-Velert, Carmen; Beltran-Carrillo, Vicente J.; Tomas, Jose Manuel

    2012-01-01

    This study examined the relationship between socio-demographic factors, screen media time usage, and light, moderate and vigorous activities on weekdays and weekends. Cross-sectional data was collected from 323 Spanish adolescents (mean age 13.59 years) who completed an interview administered recall questionnaire. Structural equation models…

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

    PubMed

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

    2016-05-01

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

  13. A New Versatile Microarray-based Method for High Throughput Screening of Carbohydrate-active Enzymes*

    PubMed Central

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

    2015-01-01

    Carbohydrate-active enzymes have multiple biological roles and industrial applications. Advances in genome and transcriptome sequencing together with associated bioinformatics tools have identified vast numbers of putative carbohydrate-degrading and -modifying enzymes including glycoside hydrolases and lytic polysaccharide monooxygenases. However, there is a paucity of methods for rapidly screening the activities of these enzymes. By combining the multiplexing capacity of carbohydrate microarrays with the specificity of molecular probes, we have developed a sensitive, high throughput, and versatile semiquantitative enzyme screening technique that requires low amounts of enzyme and substrate. The method can be used to assess the activities of single enzymes, enzyme mixtures, and crude culture broths against single substrates, substrate mixtures, and biomass samples. Moreover, we show that the technique can be used to analyze both endo-acting and exo-acting glycoside hydrolases, polysaccharide lyases, carbohydrate esterases, and lytic polysaccharide monooxygenases. We demonstrate the potential of the technique by identifying the substrate specificities of purified uncharacterized enzymes and by screening enzyme activities from fungal culture broths. PMID:25657012

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

    PubMed

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

    2015-04-01

    Carbohydrate-active enzymes have multiple biological roles and industrial applications. Advances in genome and transcriptome sequencing together with associated bioinformatics tools have identified vast numbers of putative carbohydrate-degrading and -modifying enzymes including glycoside hydrolases and lytic polysaccharide monooxygenases. However, there is a paucity of methods for rapidly screening the activities of these enzymes. By combining the multiplexing capacity of carbohydrate microarrays with the specificity of molecular probes, we have developed a sensitive, high throughput, and versatile semiquantitative enzyme screening technique that requires low amounts of enzyme and substrate. The method can be used to assess the activities of single enzymes, enzyme mixtures, and crude culture broths against single substrates, substrate mixtures, and biomass samples. Moreover, we show that the technique can be used to analyze both endo-acting and exo-acting glycoside hydrolases, polysaccharide lyases, carbohydrate esterases, and lytic polysaccharide monooxygenases. We demonstrate the potential of the technique by identifying the substrate specificities of purified uncharacterized enzymes and by screening enzyme activities from fungal culture broths. PMID:25657012

  15. Screening of halophilic bacteria and Alteromonas species for organophosphorus hydrolyzing enzyme activity.

    PubMed

    DeFrank, J J; Beaudry, W T; Cheng, T C; Harvey, S P; Stroup, A N; Szafraniec, L L

    1993-06-01

    Previously, a G-type nerve agent degrading enzyme activity was found in a halophilic bacterial isolate designated JD6.5. This organism was tentatively identified as an unknown species of the genus Alteromonas. In order to determine whether this type of enzyme activity was common in other species of Alteromonas, a screening program was initiated. A number of Alteromonas species and five halophilic bacterial isolates were cultured and their crude cell extracts screened for hydrolytic activity against several organophosphorus chemical agents and other related compounds. The samples were also screened for cross-reactivity with a monoclonal antibody raised against the purified enzyme from JD6.5 and for hybridization with a DNA probe based on its N-terminal amino acid sequence A wide spectrum of activities and reactivities were seen, suggesting a significant heterogeneity between the functionally similar enzymes that are present in these bacterial species. Enzymes of the type described here have considerable potential for the decontamination and demilitarization of chemical warfare agents. PMID:8393735

  16. Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.

    PubMed

    Nevin, Daniel K; Peters, Martin B; Carta, Giorgio; Fayne, Darren; Lloyd, David G

    2012-06-14

    We describe a fully customizable and integrated target-specific "tiered" virtual screening approach tailored to identifying and characterizing novel peroxisome proliferator activated receptor γ (PPARγ) scaffolds. Built on structure- and ligand-based computational techniques, a consensus protocol was developed for use in the virtual screening of chemical databases, focused toward retrieval of novel bioactive chemical scaffolds for PPARγ. Consequent from application, three novel PPAR scaffolds displaying distinct chemotypes have been identified, namely, 5-(4-(benzyloxy)-3-chlorobenzylidene)dihydro-2-thioxopyrimidine-4,6(1H,5H)-dione (MDG 548), 3-((4-bromophenoxy)methyl)-N-(4-nitro-1H-pyrazol-1-yl)benzamide (MDG 559), and ethyl 2-[3-hydroxy-5-(5-methyl-2-furyl)-2-oxo-4-(2-thienylcarbonyl)-2,5-dihydro-1H-pyrrol-1-yl]-4-methyl-1,3-thiazole-5-carboxylate (MDG 582). Fluorescence polarization(FP) and time resolved fluorescence resonance energy transfer (TR-FRET) show that these compounds display high affinity competitive binding to the PPARγ-LBD (EC(50) of 215 nM to 5.45 μM). Consequent characterization by a TR-FRET activation reporter assay demonstrated agonism of PPARγ by all three compounds (EC(50) of 467-594 nM). Additionally, differential PPAR isotype specificity was demonstrated through assay against PPARα and PPARδ subtypes. This work showcases the ability of target specific "tiered screen" protocols to successfully identify novel scaffolds of individual receptor subtypes with greater efficacy than isolated screening methods. PMID:22582973

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

    NASA Astrophysics Data System (ADS)

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

    2016-01-01

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

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

    PubMed

    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. PMID:24311867

  19. Whole-organism screening for gluconeogenesis identifies activators of fasting metabolism

    PubMed Central

    Gut, Philipp; Baeza-Raja, Bernat; Andersson, Olov; Hasenkamp, Laura; Hsiao, Joseph; Hesselson, Daniel; Akassoglou, Katerina; Verdin, Eric; Hirschey, Matthew D.; Stainier, Didier Y.R.

    2012-01-01

    Improving the control of energy homeostasis can lower cardiovascular risk in metabolically compromised individuals. To identify new regulators of whole-body energy control, we conducted a high-throughput screen in transgenic reporter zebrafish for small molecules that modulate the expression of the fasting-inducible gluconeogenic gene pck1. We show that this in vivo strategy identified several drugs that impact gluconeogenesis in humans, as well as metabolically uncharacterized compounds. Most notably, we find that the Translocator Protein (TSPO) ligands PK 11195 and Ro5-4864 are glucose lowering agents despite a strong inductive effect on pck1 expression. We show that these drugs are activators of a fasting-like energy state, and importantly that they protect high-fat diet induced obese mice from hepatosteatosis and glucose intolerance, two pathological manifestations of metabolic dysregulation. Thus, using a whole-organism screening strategy, this study has identified new small molecule activators of fasting metabolism. PMID:23201900

  20. REAL TIME DATA FOR REMEDIATION ACTIVITIES [11505

    SciTech Connect

    BROCK CT

    2011-01-13

    Health physicists from the CH2M HILL Plateau Remediation Company collaborated with Berkeley Nucleonics Corporation to modify the SAM 940 isotope identifier instrument to be used for nuclear waste remediation. These modifications coupled with existing capabilities of the SAM 940 have proven to be invaluable during remediation activities, reducing disposal costs by allowing swift remediation of targeted areas that have been identified as having isotopes of concern (IOC), and eliminating multiple visits to sites by declaring an excavation site clear of IOCs before demobilizing from the site. These advantages are enabled by accumulating spectral data for specific isotopes that is nearly 100 percent free of false positives, which are filtered out in 'real time.'

  1. Screening youth for suicide risk in medical settings: time to ask questions.

    PubMed

    Horowitz, Lisa M; Bridge, Jeffrey A; Pao, Maryland; Boudreaux, Edwin D

    2014-09-01

    This paper focuses on the National Action Alliance for Suicide Prevention's Research Prioritization Task Force's Aspirational Goal 2 (screening for suicide risk) as it pertains specifically to children, adolescents, and young adults. Two assumptions are forwarded: (1) strategies for screening youth for suicide risk need to be tailored developmentally; and (2) we must use instruments that were created and tested specifically for suicide risk detection and developed specifically for youth. Recommendations for shifting the current paradigm include universal suicide screening for youth in medical settings with validated instruments. PMID:25145735

  2. Active screen plasma surface modification of polycaprolactone to improve cell attachment.

    PubMed

    Fu, Xin; Sammons, Rachel L; Bertóti, Imre; Jenkins, Mike J; Dong, Hanshan

    2012-02-01

    To tailor polycaprolactone (PCL) surface properties for biomedical applications, film samples of PCL were surface modified by the active screen plasma nitriding (ASPN) technique. The chemical composition and structure were characterized by Fourier transform infrared spectroscopy and X-ray photoelectron spectroscopy. The wettability of the surface modified polymers was investigated by contact angle and surface energy methods. Biocompatibility of the prepared PCL samples was evaluated in vitro using MC3T3-E1 osteoblast-like cells. The degradability was assessed by determining the self-degradation rate (catalyzed by lipase). The results show that ASPN surface modification can effectively improve osteoblast cell adhesion and spreading on the surface of PCL. The main change in chemical composition is the exchange of some carboxyl groups on the surface for hydroxyl groups. The active-screen plasma nitriding technique has been found to be an effective and practical method to effectively improve osteoblast cell adhesion and spreading on the PCL surface. Such changes have been attributed to the increase in wettablity and generation of new hydroxyl groups by plasma treatment. After active-screen plasma treatment, the PCL film is still degradable, but the enzymatic degradation rate is slower compared with untreated PCL film. PMID:22179939

  3. Current in vitro high throughput screening approaches to assess nuclear receptor activation.

    PubMed

    Raucy, Judy L; Lasker, Jerome M

    2010-11-01

    The screening of new drug candidates for nuclear receptor activation can identify agents with the potential to produce drug-drug interactions or elicit adverse drug effects. The nuclear receptors of interest are those that control the expression of drug metabolizing enzymes and drug transporters, and include the constitutive androstane receptor (CAR, NR1I3), the pregnane X receptor (PXR, NR1I2) and the aryl hydrocarbon receptor (AhR). This review will focus on the methods currently used to assess activation of these receptors. Assessment of nuclear receptor activation can be accomplished using direct or indirect approaches. Indirect methods quantify specific gene products that result from nuclear receptor activation while direct approaches measure either the binding of ligands to the receptors or the transcriptional events produced by ligand binding. Assays that directly quantify nuclear receptor activation are growing in popularity and, importantly, are amenable to high throughput screening (HTS). Several ligand binding assays are currently being utilized, including radioligand competition binding, where compounds compete with radiolabelled ligand for binding to PXR or CAR, such as the scintillation proximity binding assay that measures the reaction of ligands with receptor-coated beads. A fluorescence resonance energy transfer assay has also been developed, where the fluorescent signal is generated via the ligand-dependent interaction between the fluorescently-labeled ligand binding domain of a nuclear receptor and co-activator proteins. Other in vitro activation assays include transient- and stably-transfected cell lines incorporating an expression vector for PXR, CAR or AhR plus a reporter gene vector containing response elements. The methods focused on in this review will be limited to the more direct in vitro approaches that are amenable to high throughput screening. PMID:21189134

  4. Towards medicinal mechanochemistry: evolution of milling from pharmaceutical solid form screening to the synthesis of active pharmaceutical ingredients (APIs).

    PubMed

    Tan, Davin; Loots, Leigh; Friščić, Tomislav

    2016-06-14

    This overview highlights the emergent area of mechanochemical reactions for making active pharmaceutical ingredients (APIs), and covers the latest advances in the recently established area of mechanochemical screening and synthesis of pharmaceutical solid forms, specifically polymorphs, cocrystals, salts and salt cocrystals. We also provide an overview of the most recent developments in pharmaceutical uses of mechanochemistry, including real-time reaction monitoring, techniques for polymorph control and approaches for continuous manufacture using twin screw extrusion, and more. Most importantly, we show how the overlap of previously unrelated areas of mechanochemical screening for API solid forms, organic synthesis by milling, and mechanochemical screening for molecular recognition, enables the emergence of a new research discipline in which different aspects of pharmaceutical and medicinal chemistry are addressed through mechanochemistry rather than through conventional solution-based routes. The emergence of such medicinal mechanochemistry is likely to have a strong impact on future pharmaceutical and medicinal chemistry, as it offers not only access to materials and reactivity that are sometimes difficult or even impossible to access from solution, but can also provide a general answer to the demands of the pharmaceutical industry for cleaner, safer and efficient synthetic solutions. PMID:27185190

  5. Time to Work or Time to Play: The Effect of Student Employment on Homework, Housework, Screen Time, and Sleep. Working Paper 423

    ERIC Educational Resources Information Center

    Kalenkoski, Charlene Marie; Pabilonia, Sabrina Wulff

    2009-01-01

    Recent research suggests that working while in high school reduces the amount of time students spend doing homework. However, an additional hour of work leads to a reduction in homework by much less than one hour, suggesting a reduction in other activities. This paper uses data from the 2003-2007 American Time Use Surveys (ATUS) to investigate the…

  6. Optimization Study of Pulsed DC Nitrogen-Hydrogen Plasma in the Presence of an Active Screen Cage

    NASA Astrophysics Data System (ADS)

    Saeed, A.; W. Khan, A.; F., Jan; U. Shah, H.; Abrar, M.; Zaka-Ul-Islam, M.; Khalid, M.; Zakaullah, M.

    2014-05-01

    A glow discharge plasma nitriding reactor in the presence of an active screen cage is optimized in terms of current density, filling pressure and hydrogen concentrations using optical emission spectroscopy (OES). The samples of AISI 304 are nitrided for different treatment times under optimum conditions. The treated samples were analyzed by X-ray diffraction (XRD) to explore the changes induced in the crystallographic structure. The XRD pattern confirmed the formation of iron and chromium nitrides arising from incorporation of nitrogen as an interstitial solid solution in the iron lattice. A Vickers microhardness tester was used to evaluate the surface hardness as a function of treatment time (h). The results showed clear evidence of improved surface hardness and a substantial amount of decrease in the treatment time compared with the previous work.

  7. Systematic screening of glycosylation- and trafficking-associated gene knockouts in Saccharomyces cerevisiae identifies mutants with improved heterologous exocellulase activity and host secretion

    PubMed Central

    2013-01-01

    Background As a strong fermentator, Saccharomyces cerevisiae has the potential to be an excellent host for ethanol production by consolidated bioprocessing. For this purpose, it is necessary to transform cellulose genes into the yeast genome because it contains no cellulose genes. However, heterologous protein expression in S. cerevisiae often suffers from hyper-glycosylation and/or poor secretion. Thus, there is a need to genetically engineer the yeast to reduce its glycosylation strength and to increase its secretion ability. Results Saccharomyces cerevisiae gene-knockout strains were screened for improved extracellular activity of a recombinant exocellulase (PCX) from the cellulose digesting fungus Phanerochaete chrysosporium. Knockout mutants of 47 glycosylation-related genes and 10 protein-trafficking-related genes were transformed with a PCX expression construct and screened for extracellular cellulase activity. Twelve of the screened mutants were found to have a more than 2-fold increase in extracellular PCX activity in comparison with the wild type. The extracellular PCX activities in the glycosylation-related mnn10 and pmt5 null mutants were, respectively, 6 and 4 times higher than that of the wild type; and the extracellular PCX activities in 9 protein-trafficking-related mutants, especially in the chc1, clc1 and vps21 null mutants, were at least 1.5 times higher than the parental strains. Site-directed mutagenesis studies further revealed that the degree of N-glycosylation also plays an important role in heterologous cellulase activity in S. cerevisiae. Conclusions Systematic screening of knockout mutants of glycosylation- and protein trafficking-associated genes in S. cerevisiae revealed that: (1) blocking Golgi-to-endosome transport may force S. cerevisiae to export cellulases; and (2) both over- and under-glycosylation may alter the enzyme activity of cellulases. This systematic gene-knockout screening approach may serve as a convenient means for

  8. Preschool Children's Exposure to Media, Technology, and Screen Time: Perspectives of Caregivers from Three Early Childcare Settings

    ERIC Educational Resources Information Center

    Sharkins, Kimberly A.; Newton, Allison B.; Albaiz, Najla Essa A.; Ernest, James M.

    2016-01-01

    Young children are being increasingly exposed to media, technology, and screen time (MeTS) at home and in instructional settings. Little is known about the long-term effects of MeTS and there is a lack of research concerning caregivers' opinions regarding young children's exposure to and utilization of MeTS. Therefore, this study explored the…

  9. Combinatorial engineering to enhance amylosucrase performance: construction, selection, and screening of variant libraries for increased activity.

    PubMed

    van der Veen, Bart A; Potocki-Véronèse, Gabrielle; Albenne, Cécile; Joucla, Gilles; Monsan, Pierre; Remaud-Simeon, Magali

    2004-02-27

    Amylosucrase is a glucosyltransferase belonging to family 13 of glycoside hydrolases and catalyses the formation of an amylose-type polymer from sucrose. Its potential use as an industrial tool for the synthesis or the modification of polysaccharides, however, is limited by its low catalytic efficiency on sucrose alone, its low stability, and its side reactions resulting in sucrose isomer formation. Therefore, combinatorial engineering of the enzyme through random mutagenesis, gene shuffling, and selective screening (directed evolution) was started, in order to generate more efficient variants of the enzyme. A convenient zero background expression cloning strategy was developed. Mutant gene libraries were generated by error-prone polymerase chain reaction (PCR), using Taq polymerase with unbalanced dNTPs or Mutazyme trade mark, followed by recombination of the PCR products by DNA shuffling. A selection method was developed to allow only the growth of amylosucrase active clones on solid mineral medium containing sucrose as the sole carbon source. Automated protocols were designed to screen amylosucrase activity from mini-cultures using dinitrosalicylic acid staining of reducing sugars and iodine staining of amylose-like polymer. A pilot experiment using the described mutagenesis, selection, and screening methods yielded two variants with significantly increased activity (five-fold under the screening conditions). Sequence analysis of these variants revealed mutations in amino acid residues which would not be considered for rational design of improved amylosucrase variants. A method for the characterisation of amylosucrase action on sucrose, consisting of accurate measurement of glucose and fructose concentrations, was introduced. This allows discrimination between hydrolysis and transglucosylation, enabling a more detailed comparison between wild-type and mutant enzymes. PMID:14988004

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

    PubMed

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

    2016-04-15

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

  11. Development and utilization of activated STAT3 detection assays for screening a library of secreted proteins.

    PubMed

    Fursov, Natalie; Gates, Irina V; Panavas, Tadas; Giles-Komar, Jill; Powers, Gordon

    2011-08-01

    Interleukin-6 (IL-6) family of cytokines are multifunctional proteins that play an important role in host defenses, acute phase reactions, immune responses, hematopoiesis, and tumorigenesis. The cytokines are produced by various lymphoid and nonlymphoid cells and mediate their biological activity through initial low-affinity binding to cell surface receptors, which are specific for their respective ligands. Ligand-specific receptor binding results in the receptor heterodimerization with ubiquitously expressed signal-transducing transmembrane component gp130 followed by activation of the gp130-associated Janus kinase, which, in turn, phosphorylates signal transducer and activator of transcription 3 (STAT3). Phosphorylated STAT3 (pSTAT3) dimerizes and translocates to the nucleus, where it activates gene transcription. Activation of STAT3 is essential to IL-6 family-associated physiological effects. Therefore, the ability to assess STAT3 phosphorylation is important for drug discovery efforts targeting IL-6 family cytokines. Various reagents and technologies are available to detect the effect of IL-6 type cytokines in treated cells. The present study describes the development of two pSTAT3 detection assays: the high-throughput screening assay based on Meso-Scale Discovery technology, which utilizes electrochemoluminescent signal measurements for the detection of pSTAT3 in treated cell extracts, and the secondary characterization assay based on fluorescent imaging analysis, which monitors pSTAT3 nuclear translocation in cells after activation. We have successfully utilized these assays to screen a small library of secreted proteins and identified inducers of STAT3 phosphorylation. The results obtained in this study demonstrate that both assays are robust, reliable, and amenable to high-throughput screening applications. PMID:21294636

  12. Preliminary Screening of Endophytic Fungi from Medicinal Plants in Malaysia for Antimicrobial and Antitumor Activity

    PubMed Central

    Radu, Son; Kqueen, Cheah Yoke

    2002-01-01

    The screening of antimicrobial activity against Gram-positive bacteria, Gram-negative bacteria, yeast and fungi was carried out on isopropanol extracts prepared from 121 isolates of endophytic fungi isolated from medicinal plants in Malaysia. Sensitivity was found to vary among the microorganisms. Bacillus subtilis, Saccharomyces cerevisiae and Alternaria sp. were susceptible to extracts from three, two and two isolates of endophytic fungi, respectively. None were found effective against Salmonella typhimurium. Sixteen endophytic fungal isolates tested were also found to exhibit antitumor activity in the yeast cell-based assay. PMID:22844221

  13. A High-Throughput Screen Reveals New Small-Molecule Activators and Inhibitors of Pantothenate Kinases

    PubMed Central

    2016-01-01

    Pantothenate kinase (PanK) is a regulatory enzyme that controls coenzyme A (CoA) biosynthesis. The association of PanK with neurodegeneration and diabetes suggests that chemical modifiers of PanK activity may be useful therapeutics. We performed a high throughput screen of >520000 compounds from the St. Jude compound library and identified new potent PanK inhibitors and activators with chemically tractable scaffolds. The HTS identified PanK inhibitors exemplified by the detailed characterization of a tricyclic compound (7) and a preliminary SAR. Biophysical studies reveal that the PanK inhibitor acts by binding to the ATP–enzyme complex. PMID:25569308

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

    PubMed

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

    2015-01-01

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

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

    PubMed Central

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

    2015-01-01

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

  16. A 96-well electrochemical method for the screening of enzymatic activities.

    PubMed

    Abdellaoui, Sofiène; Noiriel, Alexandre; Henkens, Robert; Bonaventura, Celia; Blum, Loïc J; Doumèche, Bastien

    2013-04-01

    The rapid electrochemical screening of enzyme activities in bioelectronics is still a challenging issue. In order to solve this problem, we propose to use a 96-well electrochemical assay. This system is composed of 96 screen-printed electrodes on a printed circuit board adapted from a commercial system (carbon is used as the working electrode and silver chloride as the counter/reference electrode). The associated device allows for the measurements on the 96 electrodes to be performed within a few seconds. In this work, we demonstrate the validity of the screening method with the commercial laccase from the fungus Trametes versicolor. The signal-to-noise ratio (S/N) is found to be the best way to analyze the electrochemical signals. The S/N follows a saturation-like mechanism with a dynamic linear range of two decades ranging from 0.5 to 75 ng of laccase (corresponding to enzymatic activities from 62 × 10(-6) to 9.37 × 10(-3) μmol min(-1)) and a sensitivity of 3027 μg(-1) at +100 mV versus Ag/AgCl. Laccase inhibitors (azide and fluoride anions), pH optima, and interfering molecules could also be identified within a few minutes. PMID:23461701

  17. Screening for Suitable Reference Genes for Quantitative Real-Time PCR in Heterosigma akashiwo (Raphidophyceae).

    PubMed

    Ji, Nanjing; Li, Ling; Lin, Lingxiao; Lin, Senjie

    2015-01-01

    The raphidophyte Heterosigma akashiwo is a globally distributed harmful alga that has been associated with fish kills in coastal waters. To understand the mechanisms of H. akashiwo bloom formation, gene expression analysis is often required. To accurately characterize the expression levels of a gene of interest, proper reference genes are essential. In this study, we assessed ten of the previously reported algal candidate genes (rpL17-2, rpL23, cox2, cal, tua, tub, ef1, 18S, gapdh, and mdh) for their suitability as reference genes in this species. We used qRT-PCR to quantify the expression levels of these genes in H. akashiwo grown under different temperatures, light intensities, nutrient concentrations, and time points over a diel cycle. The expression stability of these genes was evaluated using geNorm and NormFinder algorithms. Although none of these genes exhibited invariable expression levels, cal, tub, rpL17-2 and rpL23 expression levels were the most stable across the different conditions tested. For further validation, these selected genes were used to normalize the expression levels of ribulose-1, 5-bisphosphate carboxylase/oxygenase large unite (HrbcL) over a diel cycle. Results showed that the expression of HrbcL normalized against each of these reference genes was the highest at midday and lowest at midnight, similar to the diel patterns typically documented for this gene in algae. While the validated reference genes will be useful for future gene expression studies on H. akashiwo, we expect that the procedure used in this study may be helpful to future efforts to screen reference genes for other algae. PMID:26133173

  18. Screening for Suitable Reference Genes for Quantitative Real-Time PCR in Heterosigma akashiwo (Raphidophyceae)

    PubMed Central

    Ji, Nanjing; Li, Ling; Lin, Lingxiao; Lin, Senjie

    2015-01-01

    The raphidophyte Heterosigma akashiwo is a globally distributed harmful alga that has been associated with fish kills in coastal waters. To understand the mechanisms of H. akashiwo bloom formation, gene expression analysis is often required. To accurately characterize the expression levels of a gene of interest, proper reference genes are essential. In this study, we assessed ten of the previously reported algal candidate genes (rpL17-2, rpL23, cox2, cal, tua, tub, ef1, 18S, gapdh, and mdh) for their suitability as reference genes in this species. We used qRT-PCR to quantify the expression levels of these genes in H. akashiwo grown under different temperatures, light intensities, nutrient concentrations, and time points over a diel cycle. The expression stability of these genes was evaluated using geNorm and NormFinder algorithms. Although none of these genes exhibited invariable expression levels, cal, tub, rpL17-2 and rpL23 expression levels were the most stable across the different conditions tested. For further validation, these selected genes were used to normalize the expression levels of ribulose-1, 5-bisphosphate carboxylase/oxygenase large unite (HrbcL) over a diel cycle. Results showed that the expression of HrbcL normalized against each of these reference genes was the highest at midday and lowest at midnight, similar to the diel patterns typically documented for this gene in algae. While the validated reference genes will be useful for future gene expression studies on H. akashiwo, we expect that the procedure used in this study may be helpful to future efforts to screen reference genes for other algae. PMID:26133173

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

    PubMed Central

    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.

    2016-01-01

    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. PMID:27457881

  20. Trichomonas vaginalis: determination of acid phosphatase activity as a pharmacological screening procedure.

    PubMed

    Martínez-Grueiro, M M; Montero-Pereira, D; Giménez-Pardo, C; Nogal-Ruiz, J J; Escario, J A; Gómez-Barrio, A

    2003-10-01

    A simple method to screen trichomonacides, based on the quantification of acid phosphatase (AP) activity, has been designed. Using p-nitrophenyl phosphate as chromogenic substrate, we first determined the optimal conditions for enzyme reaction. After seeding, a linear correlation between number of trichomonads and optical densities at 405 nm was obtained at 24 hr but not at 48 hr. Then, the inhibitory effect of metronidazole was assessed both by microscope counts and by AP determination. Similar values for 50% inhibitory concentrations (2.6 microM), with 95% confidence limits of 1.91-3.33 for microscopic and 2.21-3.05 for colorimetric method, were obtained. We concluded that the colorimetric method described in this investigation is suitable for pharmacological studies and for the screening of new, potential antitrichomonal agents. PMID:14627165

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

    PubMed

    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

    2016-01-01

    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. PMID:27457881

  2. A television in the bedroom is associated with higher weekday screen time among youth with attention deficit hyperactivity disorder (ADD/ADHD)

    PubMed Central

    Lo, Charmaine B.; Waring, Molly E.; Pagoto, Sherry L.; Lemon, Stephenie C.

    2014-01-01

    Objective A TV in the bedroom has been associated with screen time in youth. Youth with attention deficit hyperactivity disorder (ADD/ADHD) have higher rates of screen time, but associations with bedroom TVs are unknown in this population. We examined the association of having a bedroom TV with screen time among youth with ADD/ADHD. Methods Data were from the 2007 National Survey of Children's Health. Youth 6–17 years whose parent/guardian reported a physician's diagnosis of ADD/ADHD (n = 7024) were included in the analysis. Parents/guardians reported the presence of a bedroom TV and average weekday TV screen time. Multivariate linear and logistic regression models assessed the effects of a bedroom on screen time. Results Youth with ADD/ADHD engaged in screen time with an average of 149.1 min/weekday and 59% had a TV in their bedroom. Adjusting for child and family characteristics, having a TV in the bedroom was associated with 25 minute higher daily screen time (95% CI: 12.8–37.4 min/day). A bedroom TV was associated with 32% higher odds of engaging in screen time for over 2 h/day (OR = 1.3; 95% CI: 1.0–1.7). Conclusion Future research should explore whether removing TVs from bedrooms reduces screen time among youth with ADD/ADHD. PMID:25599016

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

    PubMed

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

    2011-01-01

    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. PMID:21307835

  4. Passive versus Active Parental Permission: Implications for the Ability of School-Based Depression Screening to Reach Youth at Risk

    ERIC Educational Resources Information Center

    Chartier, Maggie; Stoep, Ann Vander; McCauley, Elizabeth; Herting, Jerald R.; Tracy, Melissa; Lymp, James

    2008-01-01

    Background: Depression is prevalent among children and adolescents and often goes untreated with adverse effects on academic success and healthy development. Depression screening can facilitate early identification and timely referral to prevention and treatment programs. Conducting school-based emotional health screening, however, raises the…

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

    PubMed Central

    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

  6. Self-reported oral cancer screening by smoking status in Maryland: trends over time

    PubMed Central

    Viswanath, Archana; Kerns, Timothy J.; Sorkin, John D.; Dwyer, Diane M.; Groves, Carmela; Steinberger, Eileen K.

    2014-01-01

    Objectives The study aims to examine whether a higher proportion of current and former smokers reported having an oral cancer screening (OCS) exam in the past year compared with never smokers in Maryland between 2002 and 2008. Methods Secondary analysis of the Maryland Cancer Surveys (conducted in 2002, 2004, 2006, and 2008), population-based, random-digit-dial surveys on cancer screening among adults age 40 years and older. Of 20,197 individuals who responded to the surveys, 19,054 answered questions on OCS and smoking. Results are weighted to the Maryland population. Results Self-reported OCS in the past year increased from 33 percent in 2002 to 40 percent in 2008. Screening among never and former smokers increased from about 35 percent to 42 percent and from 35 percent to 43 percent, respectively; screening among current smokers remained between 23 percent and 25 percent. In the adjusted analysis, current smokers had decreased odds of screening compared with never smokers; no significant difference was observed between former and never smokers. When the variable dental visit in the last year was included in the adjusted analysis, it became the strongest predictor of OCS. Conclusions Between 2002 and 2008, self-reported OCS in the last year increased among former and never smokers, but remained unchanged for current smokers. A visit to a dental professional attenuated the difference in OCS between current and never smokers. Dental visit in the last year was the strongest predictor of OCS. PMID:23521183

  7. Field screening at petroleum contaminated sites: A tool to save time, money

    SciTech Connect

    Hood, G.M.; Pucel, P.G.; Allee, P.

    1998-01-01

    The most expensive part of an environmental assessment is often lab services. Control of these costs while still collecting adequate data to assess a site is sometimes the difference between solvency and bankruptcy, especially for small companies. Fortunately, the use of field screening techniques can significantly reduce the quantity of samples going to the laboratory for analysis, thus controlling overall project costs. Chemical and Environmental Consultants, Inc. (CEC) has been field evaluating a rapid, widely applicable method for field screening petroleum contaminated soils and wastes for SVOCs. The method is similar in application to US EPA Method 418.1 and allows for the field screening of soil and waste samples in about 10 minutes. The method uses fluorescence spectroscopy analysis of a solvent extract of the soil or waste sample.

  8. The generation of wear-resistant antimicrobial stainless steel surfaces by active screen plasma alloying with N and nanocrystalline Ag.

    PubMed

    Dong, Yangchun; Li, Xiaoying; Sammons, Rachel; Dong, Hanshan

    2010-04-01

    Hospital-acquired infections (HAIs), a large proportion of which are derived from contact transmission, represent a massive global challenge. In this study a novel active screen plasma (ASP) alloying technology has been developed to generate highly durable antimicrobial surfaces by combining a wear-resistant S-phase with nanocrystalline silver for medical grade stainless steel. The phase constituent, microstructure, composition and surface roughness of the alloyed surfaces were fully characterized, and the surface hardness, wear resistance and antimicrobial efficiency of the treated surfaces were evaluated. Experimental results showed that the surface hardness and sliding wear resistance of medical grade 316LVM stainless steel can be effectively improved by the ASP alloying treatment; furthermore, the Ag alloyed S-phase can achieve 93% reduction in Escherichia coli (E. coli) after 6 h contact time. Therefore, the novel ASP alloying treatment can not only improve wear resistance but also confer antibacterial activity to stainless steel surfaces. PMID:20119942

  9. [Variable magnetic field of 8 Hz corrects the opioid system activity in mollusks behind the ferromagnetic screening].

    PubMed

    Temur'iants, N A; Kostiuk, A S

    2014-01-01

    The three phases of mollusk nociception alteration as a result of extended ferromagnetic screening combined with exposure to a variable magnetic field of 8 Hz correlated with phase changes in the opioid system activity (OSA) deduced from the naloxone action on the thermal avoidance response. On phase I, OSA inactivation was inhibited and, consequently, hyperalgesia progression was expedited. On phase II, OSA rose so that naloxone annulled completely the antinociceptive effect produced by the ferromagnetic screening. On phase III, OSA declined progressively, as naloxone merely reduced the antinociceptive effect because of apparently, growing OSA tolerance to the ferromagnetic screening. Phase I was absent when mollusks were exposed to the ferromagnetic screening and variable magnetic field; however, OSA changes on phases II and III were present. It was concluded that the variable magnetic field of 8 Hz can be used for correcting changes in the opioid system activity in mollusks behind the ferromagnetic screening. PMID:25163338

  10. Pharmaceutical screen identifies novel target processes for activation of autophagy with a broad translational potential.

    PubMed

    Chauhan, Santosh; Ahmed, Zahra; Bradfute, Steven B; Arko-Mensah, John; Mandell, Michael A; Won Choi, Seong; Kimura, Tomonori; Blanchet, Fabien; Waller, Anna; Mudd, Michal H; Jiang, Shanya; Sklar, Larry; Timmins, Graham S; Maphis, Nicole; Bhaskar, Kiran; Piguet, Vincent; Deretic, Vojo

    2015-01-01

    Autophagy is a conserved homeostatic process active in all human cells and affecting a spectrum of diseases. Here we use a pharmaceutical screen to discover new mechanisms for activation of autophagy. We identify a subset of pharmaceuticals inducing autophagic flux with effects in diverse cellular systems modelling specific stages of several human diseases such as HIV transmission and hyperphosphorylated tau accumulation in Alzheimer's disease. One drug, flubendazole, is a potent inducer of autophagy initiation and flux by affecting acetylated and dynamic microtubules in a reciprocal way. Disruption of dynamic microtubules by flubendazole results in mTOR deactivation and dissociation from lysosomes leading to TFEB (transcription factor EB) nuclear translocation and activation of autophagy. By inducing microtubule acetylation, flubendazole activates JNK1 leading to Bcl-2 phosphorylation, causing release of Beclin1 from Bcl-2-Beclin1 complexes for autophagy induction, thus uncovering a new approach to inducing autophagic flux that may be applicable in disease treatment. PMID:26503418

  11. Pharmaceutical screen identifies novel target processes for activation of autophagy with a broad translational potential

    PubMed Central

    Chauhan, Santosh; Ahmed, Zahra; Bradfute, Steven B.; Arko-Mensah, John; Mandell, Michael A.; Won Choi, Seong; Kimura, Tomonori; Blanchet, Fabien; Waller, Anna; Mudd, Michal H.; Jiang, Shanya; Sklar, Larry; Timmins, Graham S.; Maphis, Nicole; Bhaskar, Kiran; Piguet, Vincent; Deretic, Vojo

    2015-01-01

    Autophagy is a conserved homeostatic process active in all human cells and affecting a spectrum of diseases. Here we use a pharmaceutical screen to discover new mechanisms for activation of autophagy. We identify a subset of pharmaceuticals inducing autophagic flux with effects in diverse cellular systems modelling specific stages of several human diseases such as HIV transmission and hyperphosphorylated tau accumulation in Alzheimer's disease. One drug, flubendazole, is a potent inducer of autophagy initiation and flux by affecting acetylated and dynamic microtubules in a reciprocal way. Disruption of dynamic microtubules by flubendazole results in mTOR deactivation and dissociation from lysosomes leading to TFEB (transcription factor EB) nuclear translocation and activation of autophagy. By inducing microtubule acetylation, flubendazole activates JNK1 leading to Bcl-2 phosphorylation, causing release of Beclin1 from Bcl-2-Beclin1 complexes for autophagy induction, thus uncovering a new approach to inducing autophagic flux that may be applicable in disease treatment. PMID:26503418

  12. Screening of plant extracts for antioxidant activity: a comparative study on three testing methods.

    PubMed

    Koleva, Irina I; van Beek, Teris A; Linssen, Jozef P H; de Groot, Aede; Evstatieva, Lyuba 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 beta-carotene bleaching test (BCBT), have been compared with regard to their application in the screening of plant extracts. The strengths and limitations of each method have been illustrated by testing a number of extracts, of differing polarity, from plants of the genus Sideritis, and two known antioxidants (butylated hydroxytoluene and rosmarinic acid). The sample polarity was important for the exhibited activity in the BCBT and HS-GC methods but not for the DPPH method. The complex composition of the extracts and partition phenomena affected their activity in each assay. The value of the BCBT method appears to be limited to less polar samples. Although slow, the HS-GC method is preferable for assessing the antioxidant inhibitory properties on the formation of unwanted secondary volatile products. Being rapid, simple and independent of sample polarity, the DPPH method is very convenient for the quick screening of many samples for radical scavenging activity. PMID:11899609

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

    PubMed Central

    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

  14. Phytochemical screening of five medicinal legumes and their evaluation for in vitro anti-tubercular activity

    PubMed Central

    Kumar, J. Komal; Devi Prasad, A. G.; Chaturvedi, Vinita

    2014-01-01

    Background: Tuberculosis is a leading cause of death in the world. A new alternative for the treatment of tuberculosis is urgently required, due to the emergence of multidrug resistant Mycobacterium tuberculosis. Aim: There is currently considerable interest in developing potential drugs from medicinal plants for treating tuberculosis. To evaluate anti-tubercular activity in the leaves of Kingiodendron pinnatum Rox. Hams., Humboldtia brunonis Wall., Indigofera cassioides Rottl.ex DC., Derris scandens Benth. and Ceasalpinia mimosoides Lamk. Materials and Methods: Non-polar and polar solvent extracts of leaves of these medicinal legumes were tested against M. tuberculosis H37RV and minimum inhibitory concentrations (MICs) were determined by the agar based proportion assay. Results: Phytochemical screening for secondary metabolites revealed the presence of saponins, steroids, anthro-quinones, terpinods, flavonoids and phlabotanins. Crude leaf extracts of these plants have shown MIC value of 50 μg/ml as against the standard drug Isoniazid value of 0.025 μg/ml. Conclusion: Results showed that crude extracts of legume leaves screened exhibited potential anti-tubercular activity against M. tuberculosis and further work is required to identify the active molecule of these legumes, to get a novel anti-tubercular drug. This is the maiden finding on anti-tubercular activity of these medicinal legumes. PMID:25364208

  15. A robust screening method for dietary agents that activate tumour-suppressor microRNAs

    PubMed Central

    Hagiwara, Keitaro; Gailhouste, Luc; Yasukawa, Ken; Kosaka, Nobuyoshi; Ochiya, Takahiro

    2015-01-01

    Certain dietary agents, such as natural products, have been reported to show anti-cancer effects. However, the underlying mechanisms of these substances in human cancer remain unclear. We recently found that resveratrol exerts an anti-cancer effect by upregulating tumour-suppressor microRNAs (miRNAs). In the current study, we aimed to identify new dietary products that have the ability to activate tumour-suppressor miRNAs and that therefore may serve as novel tools for the prevention and treatment of human cancers. We describe the generation and use of an original screening system based on a luciferase-based reporter vector for monitoring miR-200c tumour-suppressor activity. By screening a library containing 139 natural substances, three natural compounds — enoxolone, magnolol and palmatine chloride — were identified as being capable of inducing miR-200c expression in breast cancer cells at 10 μM. Moreover, these molecules suppressed the invasiveness of breast cancer cells in vitro. Next, we identified a molecular pathway by which the increased expression of miR-200c induced by natural substances led to ZEB1 inhibition and E-cadherin induction. These results indicate that our method is a valuable tool for a fast identification of natural molecules that exhibit tumour-suppressor activity in human cancer through miRNA activation. PMID:26423775

  16. A high throughput gas exchange screen for determining rates of photorespiration or regulation of C4 activity

    PubMed Central

    Bellasio, Chandra; Burgess, Steven J; Griffiths, Howard

    2014-01-01

    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. PMID:25006037

  17. Positive posttraumatic stress disorder screens among first-time medical cannabis patients: prevalence and association with other substance use.

    PubMed

    Bohnert, Kipling M; Perron, Brian E; Ashrafioun, Lisham; Kleinberg, Felicia; Jannausch, Mary; Ilgen, Mark A

    2014-10-01

    Twenty-one states and the District of Columbia have passed legislation allowing for the use of medical cannabis for those individuals with qualifying medical conditions, which include posttraumatic stress disorder (PTSD) for a growing number of states. Little information is available regarding PTSD among medical cannabis patients. This study seeks to provide initial data on this topic by examining the prevalence and correlates of positive PTSD screens among a sample of patients seeking medical cannabis certification for the first time (n=186). Twenty-three percent (42/186; 95% confidence interval [CI] =17%-29%) of the patients in the study sample screened positive for PTSD. Moreover, the group that screened positive for PTSD had higher percentages of lifetime prescription opioid, cocaine, prescription sedative, and street opioid use, as well as a higher percentage of recent prescription sedative use, than the group that screened negative for PTSD. These findings highlight the relatively common use of other substances among medical cannabis patients with significant PTSD symptoms, even when compared with other patients seeking medical cannabis for the first time. As a growing number of states include PTSD among the list of qualifying medical conditions for medical cannabis, additional research is needed to better characterize the longitudinal relationship between medical cannabis use and PTSD symptoms. PMID:24930048

  18. Rare earth phosphors and phosphor screens

    DOEpatents

    Buchanan, Robert A.; Maple, T. Grant; Sklensky, Alden F.

    1981-01-01

    This invention relates to rare earth phosphor screens for converting image carrying incident radiation to image carrying visible or near-visible radiation and to the rare earth phosphor materials utilized in such screens. The invention further relates to methods for converting image carrying charged particles to image carrying radiation principally in the blue and near-ultraviolet region of the spectrum and to stabilized rare earth phosphors characterized by having a continuous surface layer of the phosphors of the invention. More particularly, the phosphors of the invention are oxychlorides and oxybromides of yttrium, lanthanum and gadolinium activated with trivalent cerium and the conversion screens are of the type illustratively including x-ray conversion screens, image amplifier tube screens, neutron imaging screens, cathode ray tube screens, high energy gamma ray screens, scintillation detector screens and screens for real-time translation of image carrying high energy radiation to image carrying visible or near-visible radiation.

  19. Trainable structure-activity relationship model for virtual screening of CYP3A4 inhibition.

    PubMed

    Didziapetris, Remigijus; Dapkunas, Justas; Sazonovas, Andrius; Japertas, Pranas

    2010-11-01

    A new structure-activity relationship model predicting the probability for a compound to inhibit human cytochrome P450 3A4 has been developed using data for >800 compounds from various literature sources and tested on PubChem screening data. Novel GALAS (Global, Adjusted Locally According to Similarity) modeling methodology has been used, which is a combination of baseline global QSAR model and local similarity based corrections. GALAS modeling method allows forecasting the reliability of prediction thus defining the model applicability domain. For compounds within this domain the statistical results of the final model approach the data consistency between experimental data from literature and PubChem datasets with the overall accuracy of 89%. However, the original model is applicable only for less than a half of PubChem database. Since the similarity correction procedure of GALAS modeling method allows straightforward model training, the possibility to expand the applicability domain has been investigated. Experimental data from PubChem dataset served as an example of in-house high-throughput screening data. The model successfully adapted itself to both data classified using the same and different IC₅₀ threshold compared with the training set. In addition, adjustment of the CYP3A4 inhibition model to compounds with a novel chemical scaffold has been demonstrated. The reported GALAS model is proposed as a useful tool for virtual screening of compounds for possible drug-drug interactions even prior to the actual synthesis. PMID:20814717

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

    PubMed

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

    2015-10-28

    Sensitive assay of tyrosinase (TYR) activity is in urgent demand for both fundamental research and practical application, but the exploration of functional materials with good biocompatibility for its activity evaluation at the intracellular level is still challenging until now. In this work, we develop a convenient and real-time assay with high sensitivity for TYR activity/level monitoring and its inhibitor screening based on biocompatible dopamine functionalized carbon quantum dots (Dopa-CQDs). Dopamine with redox property was functionalized on the surface of carbon quantum dots to construct a Dopa-CQDs conjugate with strong bluish green fluorescence. When the dopamine moiety in Dopa-CQDs conjugate was oxidized to a dopaquinone derivative under specific catalysis of TYR, an intraparticle photoinduced electron transfer (PET) process between CQDs and dopaquinone moiety took place, and then the fluorescence of the conjugate could be quenched simultaneously. Quantitative evaluation of TYR activity was established in terms of the relationship between fluorescence quenching efficiency and TYR activity. The assay covered a broad linear range of up to 800 U/L with a low detection limit of 7.0 U/L. Arbutin, a typical inhibitor of TYR, was chosen as an example to assess its function of inhibitor screening, and positive results were observed that fluorescence quenching extent of the probe was reduced in the presence of arbutin. It is also demonstrated that Dopa-CQD conjugate possesses excellent biocompatibility, and can sensitively monitor intracellular tyrosinase level in melanoma cells and intracellular pH changes in living cells, which provides great potential in application of TYR/pH-associated disease monitoring and medical diagnostics. PMID:26440479

  1. Activity-Based Metagenomic Screening and Biochemical Characterization of Bovine Ruminal Protozoan Glycoside Hydrolases▿†

    PubMed Central

    Findley, Seth D.; Mormile, Melanie R.; Sommer-Hurley, Andrea; Zhang, Xue-Cheng; Tipton, Peter; Arnett, Krista; Porter, James H.; Kerley, Monty; Stacey, Gary

    2011-01-01

    The rumen, the foregut of herbivorous ruminant animals such as cattle, functions as a bioreactor to process complex plant material. Among the numerous and diverse microbes involved in ruminal digestion are the ruminal protozoans, which are single-celled, ciliated eukaryotic organisms. An activity-based screen was executed to identify genes encoding fibrolytic enzymes present in the metatranscriptome of a bovine ruminal protozoan-enriched cDNA expression library. Of the four novel genes identified, two were characterized in biochemical assays. Our results provide evidence for the effective use of functional metagenomics to retrieve novel enzymes from microbial populations that cannot be maintained in axenic cultures. PMID:21948825

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

    PubMed

    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). PMID:26408890

  3. Screening of Different Extracts from Artemisia Species for Their Potential Antimalarial Activity

    PubMed Central

    Mojarrab, Mahdi; Naderi, Rozhin; Heshmati Afshar, Fariba

    2015-01-01

    The formation of hemozoin (malaria pigment) has been proposed as an ideal drug target for antimalarial screening programs. In this study, we used an improved, cost-effective and high-throughput spectrophotometric assay to screen plant extracts for finding novel antimalarial plant sources. Fifteen extracts with different polarity from three Iranian Artemisia species, A. ciniformis, A. biennis and A. turanica, were assessed for their antimalarial activity by in-vitro β-hematin formation assay. The most potent effect was observed in dichloromethane (DCM) extract of A. ciniformis with IC50 and IC90 values of 0.92 ± 0.01 and 1.29 ± 0.02 mg/mL, respectively. Ethyl acetate (EtOAC) extracts of A. biennis and A. turanica also showed significant antimalarial activities with IC50 values of 1.11 ± 0.02 and 1.35 ± 0.08 mg/mL and IC90 values of 1.22 ± 0.04 and 2.81 ± 0.21 mg/mL, respectively. Based on these results, it is possible to conclude that the components with strong antimalarial activity have been concentrated in the medium-polar extracts. PMID:25901169

  4. Exploring the structure-activity relationships of ABCC2 modulators using a screening approach.

    PubMed

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

    2015-07-01

    ABCC2 is a transporter with key influence on liver and kidney pharmacokinetics. In order to explore the structure-activity relationships of compounds that modulate ABCC2, and by doing so gain insights into drug-drug interactions, we screened a library of 432 compounds for modulators of radiolabeled β-estradiol 17-(β-d-glucuronide) (EG) and fluorescent 5(6)-carboxy-2',7'-dichlorofluorescein transport (CDCF) in membrane vesicles. Following the primary screen at 80μM, dose-response curves were used to investigate in detail 86 compounds, identifying 16 low μM inhibitors and providing data about the structure-activity relationships in four series containing 19, 24, 10, and eight analogues. Measurements with the CDCF probe were consistently more robust than for the EG probe. Only one compound was clearly probe-selective with a 50-fold difference in the IC50s obtained by the two assays. We built 24 classification models using the SVM and fused-XY Kohonen methods, revealing molecular descriptors related to number of rings, solubility and lipophilicity as important to distinguish inhibitors from inactive compounds. This study is to the best of our knowledge the first to provide details about structure-activity relationships in ABCC2 modulation. PMID:25935289

  5. High-content screening assay for identification of chemicals impacting spontaneous activity in zebrafish embryos.

    PubMed

    Raftery, Tara D; Isales, Gregory M; Yozzo, Krystle L; Volz, David C

    2014-01-01

    Although cell-based assays exist, rapid and cost-efficient high-content screening (HCS) assays within intact organisms are needed to support prioritization for developmental neurotoxicity testing in rodents. During zebrafish embryogenesis, spontaneous tail contractions occur from late-segmentation (∼19 h postfertilization, hpf) through early pharyngula (∼29 hpf) and represent the first sign of locomotion. Using transgenic zebrafish (fli1:egfp) that stably express eGFP beginning at ∼14 hpf, we have developed and optimized a 384-well-based HCS assay that quantifies spontaneous activity within single zebrafish embryos after exposure to test chemicals in a concentration-response format. Following static exposure of one embryo per well from 5 to 25 hpf, automated image acquisition procedures and custom analysis protocols were used to quantify total body area and spontaneous activity in live embryos. Survival and imaging success rates across control plates ranged from 87.5 to 100% and 93.3-100%, respectively. Using our optimized procedures, we screened 16 chemicals within the US EPA's ToxCast Phase-I library, and found that exposure to abamectin and emamectin benzoate-both potent avermectins-abolished spontaneous activity in the absence of gross malformations. Overall, compared to existing locomotion-based zebrafish assays conducted later in development, this method provides a simpler discovery platform for identifying potential developmental neurotoxicants. PMID:24328182

  6. In vivo RNAi screen identifies NLK as a negative regulator of mesenchymal activity in glioblastoma

    PubMed Central

    Cho, Hee Jin; Lee, Jin-Ku; Kim, Gi-Soo; Han, Suji; Kim, Woon Jin; Shin, Yong Jae; Joo, Kyeung Min; Paddison, Patrick J.; Ishitani, Tohru; Lee, Jeongwu; Nam, Do-Hyun

    2015-01-01

    Glioblastoma (GBM) is the most lethal brain cancer with profound genomic alterations. While the bona fide tumor suppressor genes such as PTEN, NF1, and TP53 have high frequency of inactivating mutations, there may be the genes with GBM-suppressive roles for which genomic mutation is not a primary cause for inactivation. To identify such genes, we employed in vivo RNAi screening approach using the patient-derived GBM xenograft models. We found that Nemo-Like Kinase (NLK) negatively regulates mesenchymal activities, a characteristic of aggressive GBM, in part via inhibition of WNT/β-catenin signaling. Consistent with this, we found that NLK expression is especially low in a subset of GBMs that harbors high WNT/mesenchymal activities. Restoration of NLK inhibited WNT and mesenchymal activities, decreased clonogenic growth and survival, and impeded tumor growth in vivo. These data unravel a tumor suppressive role of NLK and support the feasibility of combining oncogenomics with in vivo RNAi screen. PMID:26023737

  7. Comparative screening of plant essential oils: phenylpropanoid moiety as basic core for antiplatelet activity.

    PubMed

    Tognolini, M; Barocelli, E; Ballabeni, V; Bruni, R; Bianchi, A; Chiavarini, M; Impicciatore, M

    2006-02-23

    Essential oils extracted from different plants (Anthemis nobilis L., Artemisia dracunculus L., Cannabis sativa L., Cupressus sempervirens L., Cymbopogon citratus (DC.) Stapf., Curcuma longa L., Foeniculum vulgare L., Hypericum perforatum L., Hyssopus officinalis L., Mentha spicata L., Monarda didyma L., Ocimum basilicum L., Ocotea quixos Kosterm., Origanum vulgare L., Pinus nigra J.F. Arnold, Pinus silvestris L., Piper crassinervium Kunth., Rosmarinus officinalis L., Salvia officinalis L., Salvia sclarea L., Santolina chamaecyparissus L., Thymus vulgaris L., Zingiber officinaie L.) were screened in guinea pig and rat plasma in order to assess antiplatelet activity and inhibition of clot retraction. The oils were chemically analysed and a relationship between components and ability to affect hemostasis was evidenced. O. quixos, F. vulgaris, and A. dracunculus showed the highest antiplatelet activity against ADP, Arachidonic Acid and the Thromboxane A2 agonist U46619 (IC50, 4-132 microg ml(-1)), and a good ability to destabilize clot retraction (IC50, 19-180 microg ml(-1)). For these oils a significant correlation between antiplatelet potency and phenylpropanoids content (54-86%) was evidenced thus suggesting a key role for this moiety in the prevention of clot formation. These findings provide the rationale to take in account the antiplatelet activity in the pharmacological screening of natural products containing phenylpropanoids. PMID:16274702

  8. Cellulase activity screening using pure carboxymethylcellulose: application to soluble cellulolytic samples and to plant tissue prints.

    PubMed

    Johnsen, Hanne R; Krause, Kirsten

    2014-01-01

    Reliable, rapid and inexpensive detection of cellulolytic enzymes that can be used for a wide variety of biological and environmental samples are currently in high demand. Here, a new cellulase detection protocol is described that circumvents problems observed with popular agar-based methods by exploiting the ability of carboxymethylcellulose (CMC) to form gel-like surfaces on its own. These pure CMC-layers are sensitive to cellulolytic degradation and stainable by Gram's iodine without showing unwelcome reactions with other enzymes. The staining intensity negatively correlates with the enzyme activity and can be used for quantification. Cellulase activities are not obstructed by high sugar contents (e.g., in plant material) which limit the applicability of other quantification methods, making our new method particularly attractive for screening of plant extracts. A useful variant of this new method is its applicability to plant tissue prints for spatial mapping of the cellulolytic activity in a zymogram-like fashion. PMID:24413752

  9. Screening and HPLC-Based Activity Profiling for New Antiprotozoal Leads from European Plants

    PubMed Central

    Zimmermann, Stefanie; Thomi, Semira; Kaiser, Marcel; Hamburger, Matthias; Adams, Michael

    2012-01-01

    Based on a survey of remedies used in Renaissance Europe to treat malaria, we prepared and screened a library of 254 extracts from 61 plants for antiplasmodial activity in vitro. HPLC-based activity profiling was performed for targeted identification of active constituents in extracts. One of the most remarkable results was the identification of onopordopicrin, a germacranolide sesquiterpene lactone isolated from Arctium nemorosum as a potent inhibitor of P. falciparum with an IC50 of 6.9 μM. It was tested similarly against Trypanosoma brucei rhodesiense, the parasite which causes African sleeping sickness. With an IC50 of 0.37 μM, onopordopicrin was one of the most potent natural products reported so far. Cytotoxicity was determined against rat myoblast L6 cells (IC50: 3.06). PMID:22396915

  10. Screening of Panamanian Plants for Cosmetic Properties, and HPLC-Based Identification of Constituents with Antioxidant and UV-B Protecting Activities

    PubMed Central

    Guldbrandsen, Niels; De Mieri, Maria; Gupta, Mahabir; Liakou, Eleni; Pratsinis, Harris; Kletsas, Dimitris; Chaita, Eliza; Aligiannis, Nektarios; Skaltsounis, Alexios-Leandros; Hamburger, Matthias

    2015-01-01

    A library of 600 taxonomically diverse Panamanian plant extracts was screened for DPPH scavenging and UV-B protective activities, and the methanolic extracts of Mosquitoxylum jamaicense, Combretum cacoucia, and Casearia commersionia were submitted to HPLC-based activity profiling. The compounds located in the active time windows were isolated and identified as gallic acid derivatives and flavonoids. Gallic acid methyl ester (3) and digallic acid derivatives (2, 6) showed the highest DPPH scavenging activity (<10 μg/mL), while protocatechuic acid (7) and isoquercitrin (10) exhibited the highest UV-B protective properties. PMID:26839809

  11. Screening of Panamanian Plants for Cosmetic Properties, and HPLC-Based Identification of Constituents with Antioxidant and UV-B Protecting Activities.

    PubMed

    Guldbrandsen, Niels; De Mieri, Maria; Gupta, Mahabir; Liakou, Eleni; Pratsinis, Harris; Kletsas, Dimitris; Chaita, Eliza; Aligiannis, Nektarios; Skaltsounis, Alexios-Leandros; Hamburger, Matthias

    2015-01-01

    A library of 600 taxonomically diverse Panamanian plant extracts was screened for DPPH scavenging and UV-B protective activities, and the methanolic extracts of Mosquitoxylum jamaicense, Combretum cacoucia, and Casearia commersionia were submitted to HPLC-based activity profiling. The compounds located in the active time windows were isolated and identified as gallic acid derivatives and flavonoids. Gallic acid methyl ester (3) and digallic acid derivatives (2, 6) showed the highest DPPH scavenging activity (<10 μg/mL), while protocatechuic acid (7) and isoquercitrin (10) exhibited the highest UV-B protective properties. PMID:26839809

  12. The Association of Screen Time, Television in the Bedroom, and Obesity among School-Aged Youth: 2007 National Survey of Children's Health

    ERIC Educational Resources Information Center

    Wethington, Holly; Pan, Liping; Sherry, Bettylou

    2013-01-01

    Background: Among school-aged youth, we sought to identify characteristics associated with (1) exceeding screen time recommendations (ie, television/videos/video games more than 2 hours/weekday), and (2) exceeding screen time recommendations, the presence of a television in the bedroom, and obesity. Methods: Using 2007 National Survey of…

  13. Performance-Based Cognitive Screening Instruments: An Extended Analysis of the Time versus Accuracy Trade-off

    PubMed Central

    Larner, Andrew J.

    2015-01-01

    Early and accurate diagnosis of dementia is key to appropriate treatment and management. Clinical assessment, including the use of cognitive screening instruments, remains integral to the diagnostic process. Many cognitive screening instruments have been described, varying in length and hence administration time, but it is not known whether longer tests offer greater diagnostic accuracy than shorter tests. Data from several pragmatic diagnostic test accuracy studies examining various cognitive screening instruments in a secondary care setting were analysed to correlate measures of test diagnostic accuracy and test duration, building on the findings of a preliminary study. High correlations which were statistically significant were found between one measure of diagnostic accuracy, area under the receiver operating characteristic curve, and surrogate measures of test duration, namely total test score and total number of test items/questions. Longer cognitive screening instruments may offer greater accuracy for the diagnosis of dementia, an observation which has possible implications for the optimal organisation of dedicated cognitive disorders clinics. PMID:26854168

  14. Time-resolved luminescence screening of antibiotics in tissue matrices without centrifugation and filtration: spiked recovery studies.

    PubMed

    Chen, Guoying; Smith, Emily; Qin, Feng; Liu, Linshu

    2006-05-01

    Analyses of chemical residues in animal tissue matrices require multistep sample preparation. To simplify this process, a methodology was developed that combines sorbent extraction and solid-matrix time-resolved luminescence (TRL); it was applied to tetracycline screening in milk. Reported here is an effort to extend its application to tissue matrices, illustrated by oxytetracycline (OTC) screening in catfish muscle. Extraction and enrichment are accomplished by immersing small C18 sorbent strips into tissue homogenates for 20 min, followed by a 3 min rinse in water and a 2 min dip in a reagent solution. After desiccation, TRL is measured directly on the sorbent surface. Tissue particulates no longer interfere via attenuation or scattering, rendering centrifugation and filtration unnecessary. The integrated TRL intensity shows a linear dependence on OTC concentration in the 0-8 microg/g range (R2 = 0.9992) with a 0.026 microg/g limit of detection. To screen OTC at 2 microg/g, the U.S. regulatory tolerance level, a threshold is established at x2-3sigma2, where x2 and sigma2 are the mean and standard deviation, respectively, of the TRL signals from 15 samples fortified at 2 microg/g. Among 45 blind samples randomly fortified at 0-4 microg/g, 41 were screened correctly and 4 negative samples were presumed positive. This method has the potential to improve throughput and save assay costs by eliminating acids, organic solvents, centrifugation, and filtration. PMID:16637677

  15. Screening of Transient Receptor Potential Canonical Channel Activators Identifies Novel Neurotrophic Piperazine Compounds.

    PubMed

    Sawamura, Seishiro; Hatano, Masahiko; Takada, Yoshinori; Hino, Kyosuke; Kawamura, Tetsuya; Tanikawa, Jun; Nakagawa, Hiroshi; Hase, Hideharu; Nakao, Akito; Hirano, Mitsuru; Rotrattanadumrong, Rachapun; Kiyonaka, Shigeki; Mori, Masayuki X; Nishida, Motohiro; Hu, Yaopeng; Inoue, Ryuji; Nagata, Ryu; Mori, Yasuo

    2016-03-01

    Transient receptor potential canonical (TRPC) proteins form Ca(2+)-permeable cation channels activated upon stimulation of metabotropic receptors coupled to phospholipase C. Among the TRPC subfamily, TRPC3 and TRPC6 channels activated directly by diacylglycerol (DAG) play important roles in brain-derived neurotrophic factor (BDNF) signaling, promoting neuronal development and survival. In various disease models, BDNF restores neurologic deficits, but its therapeutic potential is limited by its poor pharmacokinetic profile. Elucidation of a framework for designing small molecules, which elicit BDNF-like activity via TRPC3 and TRPC6, establishes a solid basis to overcome this limitation. We discovered, through library screening, a group of piperazine-derived compounds that activate DAG-activated TRPC3/TRPC6/TRPC7 channels. The compounds [4-(5-chloro-2-methylphenyl)piperazin-1-yl](3-fluorophenyl)methanone (PPZ1) and 2-[4-(2,3-dimethylphenyl)piperazin-1-yl]-N-(2-ethoxyphenyl)acetamide (PPZ2) activated, in a dose-dependent manner, recombinant TRPC3/TRPC6/TRPC7 channels, but not other TRPCs, in human embryonic kidney cells. PPZ2 activated native TRPC6-like channels in smooth muscle cells isolated from rabbit portal vein. Also, PPZ2 evoked cation currents and Ca(2+) influx in rat cultured central neurons. Strikingly, both compounds induced BDNF-like neurite growth and neuroprotection, which were abolished by a knockdown or inhibition of TRPC3/TRPC6/TRPC7 in cultured neurons. Inhibitors of Ca(2+) signaling pathways, except calcineurin, impaired neurite outgrowth promotion induced by PPZ compounds. PPZ2 increased activation of the Ca(2+)-dependent transcription factor, cAMP response element-binding protein. These findings suggest that Ca(2+) signaling mediated by activation of DAG-activated TRPC channels underlies neurotrophic effects of PPZ compounds. Thus, piperazine-derived activators of DAG-activated TRPC channels provide important insights for future development of a

  16. Genome-wide siRNA screen for mediators of NF-κB activation

    PubMed Central

    Gewurz, Benjamin E.; Towfic, Fadi; Mar, Jessica C.; Shinners, Nicholas P.; Takasaki, Kaoru; Zhao, Bo; Cahir-McFarland, Ellen D.; Quackenbush, John; Xavier, Ramnik J.; Kieff, Elliott

    2012-01-01

    Although canonical NFκB is frequently critical for cell proliferation, survival, or differentiation, NFκB hyperactivation can cause malignant, inflammatory, or autoimmune disorders. Despite intensive study, mammalian NFκB pathway loss-of-function RNAi analyses have been limited to specific protein classes. We therefore undertook a human genome-wide siRNA screen for novel NFκB activation pathway components. Using an Epstein Barr virus latent membrane protein (LMP1) mutant, the transcriptional effects of which are canonical NFκB-dependent, we identified 155 proteins significantly and substantially important for NFκB activation in HEK293 cells. These proteins included many kinases, phosphatases, ubiquitin ligases, and deubiquinating enzymes not previously known to be important for NFκB activation. Relevance to other canonical NFκB pathways was extended by finding that 118 of the 155 LMP1 NF-κB activation pathway components were similarly important for IL-1β–, and 79 for TNFα–mediated NFκB activation in the same cells. MAP3K8, PIM3, and six other enzymes were uniquely relevant to LMP1-mediated NFκB activation. Most novel pathway components functioned upstream of IκB kinase complex (IKK) activation. Robust siRNA knockdown effects were confirmed for all mRNAs or proteins tested. Although multiple ZC3H-family proteins negatively regulate NFκB, ZC3H13 and ZC3H18 were activation pathway components. ZC3H13 was critical for LMP1, TNFα, and IL-1β NFκB-dependent transcription, but not for IKK activation, whereas ZC3H18 was critical for IKK activation. Down-modulators of LMP1 mediated NFκB activation were also identified. These experiments identify multiple targets to inhibit or stimulate LMP1-, IL-1β–, or TNFα–mediated canonical NFκB activation. PMID:22308454

  17. Gametocytocidal Screen Identifies Novel Chemical Classes with Plasmodium falciparum Transmission Blocking Activity

    PubMed Central

    Sanders, Natalie G.; Sullivan, David J.; Mlambo, Godfree; Dimopoulos, George; Tripathi, Abhai K.

    2014-01-01

    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. PMID:25157792

  18. Screening of some Yemeni medicinal plants for inhibitory activity against peptidases.

    PubMed

    Alasbahi, R; Melzig, M F

    2008-01-01

    Extracts of different polarities (dichloromethane, methanol, and aqueous extracts) from 5 Yemeni medicinal plants (Aspilia helianthoides, leaves; Ceropegia rupicola, whole plant; Kniphofia sumarae, whole plant; Pavetta longiflora, leaves; and Plectranthus cf barbatus, leaves) were screened for their inhibitory effects against angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), and aminopeptidase N (APN) activities. Four extracts (methanol extracts of Ceropegia rupicola, Kniphofia sumarae, and Plectranthus cf barbatus, and the aqueous extract of Pavetta longiflora) were found able to inhibit the enzymatic activity of NEP. Significant reduction in the activity of NEP (p < 0.01) was observed at a concentration of 50 microg/ml, and above of all tested extracts. The most active extract was the methanolic extract of Ceropegia rupicola with IC50 of 111 microg/ml. Only the methanolic extract of Aspilia helianthoides was found to exhibit inhibitory effect against the ACE activity with IC50 = 133 microg/ml. None of the tested plant extracts was found active against the aminopeptidase N activity. PMID:18271311

  19. Screening for Bipolar Disorder in a County Jail at the Time of Criminal Arrest

    PubMed Central

    Kemp, David E.; Hirschfeld, Robert M. A.; Ganocy, Stephen J.; Elhaj, Omar; Slembarski, Renee; Bilali, Sarah; Pontau, James; Findling, Robert L.; Calabrese, Joseph R.

    2008-01-01

    Objective This study assessed the operating characteristics of the Mood Disorder Questionnaire (MDQ) among offenders arrested and detained at a county jail. Method The MDQ, a brief self-report instrument designed to screen for all subtypes of bipolar disorder (BP I, II and NOS) was voluntarily administered to adult detainees at the Ottawa County Jail in Port Clinton, Ohio. A confirmatory diagnostic evaluation was also performed using the Mini-International Neuropsychiatric Interview (MINI). The MDQ was scored using a standard algorithm requiring endorsement of 7/13 mood items as well as two items that assess whether manic or hypomanic symptoms co-occur and cause moderate to severe functional impairment. In addition to the standard algorithm for scoring the MDQ, modifications were also tested in an attempt to improve overall sensitivity. Results Among 526 jail detainees who completed the MDQ, 37 (7%) screened positive for bipolar disorder. Of 164 detainees who agreed to a research diagnostic evaluation, 32 (19.5%) screened positive on the MDQ, while 55 (33.5%) met criteria for bipolar disorder according to the MINI. When administered to the sample of 164 adult jail detainees, the sensitivity of the MDQ was 0.47 and the specificity was 0.94. The MDQ was significantly better at detecting BP I (0.59) than BP II/NOS (0.19; p = 0.008). Modification of scoring the MDQ improved the sensitivity for detection of BP II from 0.23 to 0.54 with minimal decrease in specificity (0.84). The optimum sensitivity and specificity of the MDQ was achieved by decreasing the item threshold to 3/13 and eliminating the symptom co-occurrence and functional impairment items. Conclusion The MDQ was found to have limited utility as a screening tool for bipolar disorder in a correctional setting, particularly for the BP II subtype. PMID:17935734

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

    PubMed

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

    2015-01-01

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

  1. Electrochemical assay of α-glucosidase activity and the inhibitor screening in cell medium.

    PubMed

    Zhang, Juan; Liu, Ying; Wang, Xiaonan; Chen, Yangyang; Li, Genxi

    2015-12-15

    An electrochemical method is established in this work for the assay of α-glucosidase activity and the inhibitor screening through one-step displacement reaction, which can be directly used in cell medium. The displacement reaction can be achieved via strong binding of 4-aminophenyl-α-D-glucopyranoside (pAPG)/magnetic nanoparticles (MNPs) to pyrene boric acid (PBA) immobilized on the surface of graphite electrode (GE), compared to that of dopamine (DA)/sliver nanoparticles (AgNPs). Since α-glucosidase can specifically catalyze MNPs/pAPG into MNPs/pAP which has no binding capacity with PBA, the activity of both isolated and membrane bound enzyme can be well evaluated by using this proposed method. Meanwhile, signal amplification can be accomplished via the immobilization of DA at the outer layer of AgNPs, and the accuracy can be strengthened through magnetic separation. Moreover, this method can also be utilized for inhibitor screening not only in the medium containing the enzyme but also in cell medium. With good precision and accuracy, it may be extended to other proteases and their inhibitors as well. PMID:26201984

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

    PubMed

    Hawaze, S; Deti, H; Suleman, S

    2012-01-01

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

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

    PubMed Central

    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 Rf values that ranged from 0.05 to 0.96 for phenolic compounds and saponins. As the study is one of the first reports on the two indigenous species of Clematis; isolation, purification and characterization of the different primary and secondary metabolites may further yield alternative options to the microbial chemotherapy. PMID:23204619

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

    PubMed Central

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

    2015-01-01

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

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

    PubMed

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

    2011-04-01

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

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

    EPA Science Inventory

    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...

  7. Haida Story Telling Time with Activity Folder.

    ERIC Educational Resources Information Center

    Cogo, Robert

    One in a series of curriculum materials on Southeast Alaska Natives, this booklet contains seven myths and legends from the Haida oral tradition, each accompanied by discussion questions and suggested learning activities. Intended for use in the intermediate grades, the stories are two to four pages long with many Haida words included in the text…

  8. Qualitative validation of a liquid chromatography-quadrupole-time of flight mass spectrometry screening method for organic pollutants in waters.

    PubMed

    Diaz, R; Ibáñez, M; Sancho, J V; Hernández, F

    2013-02-01

    A multiclass wide-scope screening of organic contaminants in natural and waste water has been developed and validated for qualitative purposes, i.e. detection and reliable identification of compounds detected in samples at a certain level of concentration. The screening is based on the use of liquid chromatography coupled to quadrupole-time of flight mass spectrometry (LC-QTOF MS) and has been applied to water samples of different origin and matrix composition (surface water, ground water and effluent urban wastewater). Water samples were spiked with a standard mixture of around 150 organic contaminants from different chemical families (including a number of relevant metabolites/transformation products (TPs), at 0.1 and 1 μg/L concentration levels. After solid-phase extraction with Oasis HLB cartridges, sample extracts were analyzed by LC-QTOF MS and the accurate-mass full-spectrum data were processed for qualitative analysis. The presence of at least two ions (typically the (de)protonated molecule and one fragment ion) accurate-mass measured was used for the reliable identification. The screening detection limit (SDL) and the limit of identification (LOI) were established as the main parameters of the screening method. Nearly all compounds could be detected at the lowest concentration tested, but identification was problematic for some compounds at 0.1 μg/L level, especially in wastewater samples. The screening procedure was finally applied to different water samples using a home-made database of around 1100 organic contaminants. It allowed the detection and identification of several antibiotics, anti-inflammatory/analgesics drugs and lipid regulators. Cocaine and its metabolite benzoylecgonine were also frequently detected. In addition, triazine herbicides and their TPs, and fungicides like thiabendazol, carbendazim or imazalil, were also identified in some of the samples. PMID:23313303

  9. A Virtual Screening Approach For Identifying Plants with Anti H5N1 Neuraminidase Activity

    PubMed Central

    2016-01-01

    Recent outbreaks of highly pathogenic and occasional drug-resistant influenza strains have highlighted the need to develop novel anti-influenza therapeutics. Here, we report computational and experimental efforts to identify influenza neuraminidase inhibitors from among the 3000 natural compounds in the Malaysian-Plants Natural-Product (NADI) database. These 3000 compounds were first docked into the neuraminidase active site. The five plants with the largest number of top predicted ligands were selected for experimental evaluation. Twelve specific compounds isolated from these five plants were shown to inhibit neuraminidase, including two compounds with IC50 values less than 92 μM. Furthermore, four of the 12 isolated compounds had also been identified in the top 100 compounds from the virtual screen. Together, these results suggest an effective new approach for identifying bioactive plant species that will further the identification of new pharmacologically active compounds from diverse natural-product resources. PMID:25555059

  10. A virtual screening approach for identifying plants with anti H5N1 neuraminidase activity.

    PubMed

    Ikram, Nur Kusaira Khairul; Durrant, Jacob D; Muchtaridi, Muchtaridi; Zalaludin, Ayunni Salihah; Purwitasari, Neny; Mohamed, Nornisah; Rahim, Aisyah Saad Abdul; Lam, Chan Kit; Normi, Yahaya M; Rahman, Noorsaadah Abd; Amaro, Rommie E; Wahab, Habibah A

    2015-02-23

    Recent outbreaks of highly pathogenic and occasional drug-resistant influenza strains have highlighted the need to develop novel anti-influenza therapeutics. Here, we report computational and experimental efforts to identify influenza neuraminidase inhibitors from among the 3000 natural compounds in the Malaysian-Plants Natural-Product (NADI) database. These 3000 compounds were first docked into the neuraminidase active site. The five plants with the largest number of top predicted ligands were selected for experimental evaluation. Twelve specific compounds isolated from these five plants were shown to inhibit neuraminidase, including two compounds with IC50 values less than 92 μM. Furthermore, four of the 12 isolated compounds had also been identified in the top 100 compounds from the virtual screen. Together, these results suggest an effective new approach for identifying bioactive plant species that will further the identification of new pharmacologically active compounds from diverse natural-product resources. PMID:25555059

  11. Discovery of KDM5A inhibitors: Homology modeling, virtual screening and structure-activity relationship analysis.

    PubMed

    Wu, Xiaoai; Fang, Zhen; Yang, Bo; Zhong, Lei; Yang, Qiuyuan; Zhang, Chunhui; Huang, Shenzhen; Xiang, Rong; Suzuki, Takayoshi; Li, Lin-Li; Yang, Sheng-Yong

    2016-05-01

    Herein we report the discovery of a series of new KDM5A inhibitors. A three-dimensional (3D) structure model of KDM5A jumonji domain was firstly established based on homology modeling. Molecular docking-based virtual screening was then performed against commercial chemical databases. A number of hit compounds were retrieved. Further structural optimization and structure-activity relationship (SAR) analysis were carried out to the most active hit compound, 9 (IC50: 2.3μM), which led to the discovery of several new KDM5A inhibitors. Among them, compound 15e is the most potent one with an IC50 value of 0.22μM against KDM5A. This compound showed good selectivity for KDM5A and considerable ability to suppress the demethylation of H3K4me3 in intact cells. Compound 15e could be taken as a good lead compound for further studies. PMID:27020306

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

    PubMed

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

    2013-01-01

    A new classification method called the Optimal Bit String Tree is proposed to identify quantitative structure-activity relationships (QSARs). The method introduces the concept of a chromosome to describe the presence/absence context of a combination of descriptors. A descriptor set and its optimal chromosome form the splitting variable. A new stochastic searching scheme that contains a weighted sampling scheme, simulated annealing, and a trimming procedure optimizes the choice of splitting variable. Simulation studies and an application to screening monoamine oxidase (MAO) inhibitors show that OBSTree is advantageous in accurately and effectively identifying QSAR rules and finding different classes of active compounds. Details of the algorithm, SAS code, and simulated and real datasets are available online as supplementary materials. PMID:23878407

  13. New and simple plate test for screening relative transfructosylation activity of fungi.

    PubMed

    Dominguez, Ana; Santos, Isabel M; Teixeira, José A; Lima, Nelson

    2006-09-01

    Several microorganisms are reported to have transfructosylation activity due to fructosyltransferase and/or fructofuranosidase activities. However, the search for other fungi with higher transfructosylation activity remains a challenge. So, a presumptive and indirect colorimetric plate assay for the evaluation of transfructosylation activity in fungi was developed which involved the simultaneous determination in the same plate of glucose and fructose released from sucrose. The method entailed the (a) glucose oxidase-peroxidase coupled reaction using phenol and 4-aminoantipyrine for determination of glucose; and (b) fructose dehydrogenase oxidation in the presence of a tetrazolium salt for determination of fructose. The presence of enzymes with transfructosylation activity was identified by the formation of pink (presence of glucose) and blue (presence of fructose) halos around the fungal colony. In conclusion, the results showed that the method is suitable for screening a large number of fungi due to its simplicity, reproducibility and rapidity and also gives a relative quantitative idea of the transfructosylation activity of different fungi species. PMID:17196028

  14. Functional Screening of Hydrolytic Activities Reveals an Extremely Thermostable Cellulase from a Deep-Sea Archaeon

    PubMed Central

    Leis, Benedikt; Heinze, Simon; Angelov, Angel; Pham, Vu Thuy Trang; Thürmer, Andrea; Jebbar, Mohamed; Golyshin, Peter N.; Streit, Wolfgang R.; Daniel, Rolf; Liebl, Wolfgang

    2015-01-01

    Extreme habitats serve as a source of enzymes that 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 (8–70°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. PMID:26191525

  15. Multidimensional GPCR profiling and screening using impedance-based label-free and real-time assay.

    PubMed

    Ke, Ning; Nguyen, Khanh; Irelan, Jeffery; Abassi, Yama A

    2015-01-01

    GPCRs constitute one of the most sought-after targets in drug discovery because they are associated with conditions ranging from cardiovascular diseases, autoimmune diseases, inflammation, cancer, and diseases of the nervous system. Moreover, they are one of the most amenable targets for drug discovery because they can be modulated by small molecules, peptides, proteins, and antibodies. Therefore it may not come as a surprise that close to 40 % of the drugs that are currently on the market are targeting GPCRs. It has become evident that GPCR signaling is highly complex and may involve multiple or a subset of pathways depending on the interaction of a GPCR with an agonist or antagonist. It is imperative that any functional screening for GPCR activity integrates this complexity. In this assay protocol, we describe how the xCELLigence RTCA HT impedance-based platform which can be used for functional cell-based GPCR assays can be utilized for GPCR screening. PMID:25563187

  16. In silico approach to screen compounds active against parasitic nematodes of major socio-economic importance

    PubMed Central

    2011-01-01

    Background Infections due to parasitic nematodes are common causes of morbidity and fatality around the world especially in developing nations. At present however, there are only three major classes of drugs for treating human nematode infections. Additionally the scientific knowledge on the mechanism of action and the reason for the resistance to these drugs is poorly understood. Commercial incentives to design drugs that are endemic to developing countries are limited therefore, virtual screening in academic settings can play a vital role is discovering novel drugs useful against neglected diseases. In this study we propose to build robust machine learning model to classify and screen compounds active against parasitic nematodes. Results A set of compounds active against parasitic nematodes were collated from various literature sources including PubChem while the inactive set was derived from DrugBank database. The support vector machine (SVM) algorithm was used for model development, and stratified ten-fold cross validation was used to evaluate the performance of each classifier. The best results were obtained using the radial basis function kernel. The SVM method achieved an accuracy of 81.79% on an independent test set. Using the model developed above, we were able to indentify novel compounds with potential anthelmintic activity. Conclusion In this study, we successfully present the SVM approach for predicting compounds active against parasitic nematodes which suggests the effectiveness of computational approaches for antiparasitic drug discovery. Although, the accuracy obtained is lower than the previously reported in a similar study but we believe that our model is more robust because we intentionally employed stringent criteria to select inactive dataset thus making it difficult for the model to classify compounds. The method presents an alternative approach to the existing traditional methods and may be useful for predicting hitherto novel anthelmintic

  17. Potent Plasmodium falciparum gametocytocidal activity of diaminonaphthoquinones, lead antimalarial chemotypes identified in an antimalarial compound screen.

    PubMed

    Tanaka, Takeshi Q; Guiguemde, W Armand; Barnett, David S; Maron, Maxim I; Min, Jaeki; Connelly, Michele C; Suryadevara, Praveen Kumar; Guy, R Kiplin; Williamson, Kim C

    2015-03-01

    Forty percent of the world's population is threatened by malaria, which is caused by Plasmodium parasites and results in an estimated 200 million clinical cases and 650,000 deaths each year. Drug resistance has been reported for all commonly used antimalarials and has prompted screens to identify new drug candidates. However, many of these new candidates have not been evaluated against the parasite stage responsible for transmission, gametocytes. If Plasmodium falciparum gametocytes are not eliminated, patients continue to spread malaria for weeks after asexual parasite clearance. Asymptomatic individuals can also harbor gametocyte burdens sufficient for transmission, and a safe, effective gametocytocidal agent could also be used in community-wide malaria control programs. Here, we identify 15 small molecules with nanomolar activity against late-stage gametocytes. Fourteen are diaminonaphthoquinones (DANQs), and one is a 2-imino-benzo[d]imidazole (IBI). One of the DANQs identified, SJ000030570, is a lead antimalarial candidate. In contrast, 94% of the 650 compounds tested are inactive against late-stage gametocytes. Consistent with the ineffectiveness of most approved antimalarials against gametocytes, of the 19 novel compounds with activity against known anti-asexual-stage targets, only 3 had any strong effect on gametocyte viability. These data demonstrate the distinct biology of the transmission stages and emphasize the importance of screening for gametocytocidal activity. The potent gametocytocidal activity of DANQ and IBI coupled with their efficacy against asexual parasites provides leads for the development of antimalarials with the potential to prevent both the symptoms and the spread of malaria. PMID:25512421

  18. Potent Plasmodium falciparum Gametocytocidal Activity of Diaminonaphthoquinones, Lead Antimalarial Chemotypes Identified in an Antimalarial Compound Screen

    PubMed Central

    Tanaka, Takeshi Q; Guiguemde, W. Armand; Barnett, David S.; Maron, Maxim I.; Min, Jaeki; Connelly, Michele C.; Suryadevara, Praveen Kumar; Guy, R. Kiplin

    2014-01-01

    Forty percent of the world's population is threatened by malaria, which is caused by Plasmodium parasites and results in an estimated 200 million clinical cases and 650,000 deaths each year. Drug resistance has been reported for all commonly used antimalarials and has prompted screens to identify new drug candidates. However, many of these new candidates have not been evaluated against the parasite stage responsible for transmission, gametocytes. If Plasmodium falciparum gametocytes are not eliminated, patients continue to spread malaria for weeks after asexual parasite clearance. Asymptomatic individuals can also harbor gametocyte burdens sufficient for transmission, and a safe, effective gametocytocidal agent could also be used in community-wide malaria control programs. Here, we identify 15 small molecules with nanomolar activity against late-stage gametocytes. Fourteen are diaminonaphthoquinones (DANQs), and one is a 2-imino-benzo[d]imidazole (IBI). One of the DANQs identified, SJ000030570, is a lead antimalarial candidate. In contrast, 94% of the 650 compounds tested are inactive against late-stage gametocytes. Consistent with the ineffectiveness of most approved antimalarials against gametocytes, of the 19 novel compounds with activity against known anti-asexual-stage targets, only 3 had any strong effect on gametocyte viability. These data demonstrate the distinct biology of the transmission stages and emphasize the importance of screening for gametocytocidal activity. The potent gametocytocidal activity of DANQ and IBI coupled with their efficacy against asexual parasites provides leads for the development of antimalarials with the potential to prevent both the symptoms and the spread of malaria. PMID:25512421

  19. Optically diffracting hydrogels for screening kinase activity in vitro and in cell lysate: impact of material and solution properties.

    PubMed

    MacConaghy, Kelsey I; Chadly, Duncan M; Stoykovich, Mark P; Kaar, Joel L

    2015-03-17

    Optically diffracting films based on hydrogel-encapsulated crystalline colloidal arrays have considerable utility as sensors for detecting enzymaticphosphorylation and, thus, in screening small molecule modulators of kinases. In this work, we have investigated the impact of hydrogel properties, as well as the role of the ionic character of the surrounding environment, on the optical sensitivity of kinase responsive crystalline colloidal array-containing hydrogels. In agreement with a model of hydrogel swelling, the optical sensitivity of such materials increased as the shear modulus and the Flory-Huggins interaction parameter between polymer and solvent decreased. Additionally, elimination of extraneous charges in the polymer backbone by exploiting azide-alkyne click chemistry to functionalize the hydrogels with a peptide substrate for protein kinase A further enhanced the sensitivity of the optically diffracting films. Increasing peptide concentration and, in turn, immobilized charge within the hydrogel network was shown to increase the optical response over a range of ionic strength conditions. Ultimately, we showed that, by tuning the hydrogel and solution properties, as little as 0.1 U/μL protein kinase A could be detected in short reaction times (i.e., 2 h), which is comparable to conventional biochemical kinase assays. We further showed that this approach can be used to detect protein kinase A activity in lysate from HEK293 cells. The sensitivity of the resulting films, coupled with the advantages of photonic crystal based sensors (e.g., label free detection), makes this approach highly attractive for screening enzymatic phosphorylation. PMID:25714913

  20. Brief report: Association between socio-demographic factors, screen media usage and physical activity by type of day in Spanish adolescents.

    PubMed

    Devís-Devís, José; Peiró-Velert, Carmen; Beltrán-Carrillo, Vicente J; Tomás, José Manuel

    2012-02-01

    This study examined the relationship between socio-demographic factors, screen media time usage, and light, moderate and vigorous activities on weekdays and weekends. Cross-sectional data was collected from 323 Spanish adolescents (mean age 13.59 years) who completed an interview administered recall questionnaire. Structural equation models indicated that male and younger adolescents spent more time on vigorous activities at the weekend, while females and older adolescents showed a greater involvement in light activities both on weekdays and weekends. State school students reported engaging in light and vigorous activities for longer periods than private school students on weekends. TV viewing was negatively linked to vigorous activities during weekdays and to light and moderate activities on weekends. The amount of mobile phone usage, however, was positively linked to light activities during weekdays, but negatively on weekends. The negative relationship between adolescents' use of screen media (TV and mobile phone) and physical activity and its possible displacement, depending on the type of day, added useful comparable knowledge for policies promoting an active lifestyle. Further research is required to provide evidence of the causality in the observed relationships. PMID:21145102

  1. Detecting metabolic activities of bacteria using a simple carbon nanotube device for high-throughput screening of anti-bacterial drugs.

    PubMed

    Huang, Yinxi; Sudibya, Herry Gunadi; Chen, Peng

    2011-06-15

    In this contribution, we demonstrate a simple carbon nanotube device to electrically detect the presence of bacteria (Escherichai coli) with high sensitivity (<100 cfu/mL) and the glucose triggered metabolic activities of bacteria in real-time. As proof-of-concept demonstration, we also show that this nanoelectronic approach can be employed for high-throughput screening of anti-bacterial drugs. PMID:21570819

  2. Hollow fiber cell fishing with high-performance liquid chromatography for rapid screening and analysis of an antitumor-active protoberberine alkaloid group from Coptis chinensis.

    PubMed

    Liu, Xi; Hu, Shuang; Chen, Xuan; Bai, Xiaohong

    2014-09-01

    A novel hollow fiber cell fishing procedure with high-performance liquid chromatography (HFCF-HPLC) was developed and used for rapid screening, fishing, and analysis of bioactive compounds from traditional Chinese medicines. Human breast cancer cell MCF7, mouse breast cancer cell MADB106, and gastric cancer cell SGC7901 were seeded on the internal surface of hollow fibers that were used to screen, fish, and analyze an antitumor-active protoberberine alkaloid group from Coptis chinensis decoction. The main variables that affect the HFCF-HPLC process were investigated and optimized. The surface properties of the hollow fiber-seeded cells, cell survival rate, non-specific binding between active centers in the hollow fiber and the target compounds, repeatability, reliability, and recovery of HFCF-HPLC were investigated in detail. Several active compounds structures that were screened from Coptis chinensis by using HFCF-HPLC were identified by comparing the retention time of the reference substances. The cell membrane and cell organelle were separated from MCF7 cells for a preliminary study of the target effect of active compounds on MCF7 cells. The living cell, cell membrane, and cell organelle fishing factors of the active compound, as the indexes of drug binding ability in HFCF-HPLC, were defined and discussed. In addition, tamoxifen as positive control substance and indomethacin as negative control substance were screened by using HFCF-HPLC to further verify the method's reliability. The results demonstrated that HFCF-HPLC is an effective, rapid, stable, and reliable method to screen and analyze bioactive compounds. PMID:25023388

  3. Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

    PubMed Central

    Kawamura, Akane; Rose, Nathan R.; Ng, Stanley S.; Quinn, Amy M.; Rai, Ganesha; Mott, Bryan T.; Beswick, Paul; Klose, Robert J.; Oppermann, Udo; Jadhav, Ajit; Heightman, Tom D.; Maloney, David J.; Schofield, Christopher J.; Simeonov, Anton

    2010-01-01

    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. Nε-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. Nε-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. PMID:21124847

  4. FEATURE SCREENING FOR TIME-VARYING COEFFICIENT MODELS WITH ULTRAHIGH DIMENSIONAL LONGITUDINAL DATA

    PubMed Central

    Chu, Wanghuan; Li, Runze; Reimherr, Matthew

    2016-01-01

    Motivated by an empirical analysis of the Childhood Asthma Management Project, CAMP, we introduce a new screening procedure for varying coefficient models with ultrahigh dimensional longitudinal predictor variables. The performance of the proposed procedure is investigated via Monte Carlo simulation. Numerical comparisons indicate that it outperforms existing ones substantially, resulting in significant improvements in explained variability and prediction error. Applying these methods to CAMP, we are able to find a number of potentially important genetic mutations related to lung function, several of which exhibit interesting nonlinear patterns around puberty.

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

    PubMed Central

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

    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. PMID:23620838

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

    NASA Astrophysics Data System (ADS)

    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

  7. A high-resolution peak fractionation approach for streamlined screening of nuclear-factor-E2-related factor-2 activators in Salvia miltiorrhiza.

    PubMed

    Zhang, Hui; Luo, Li-Ping; Song, Hui-Peng; Hao, Hai-Ping; Zhou, Ping; Qi, Lian-Wen; Li, Ping; Chen, Jun

    2014-01-24

    Generation of a high-purity fraction library for efficiently screening active compounds from natural products is challenging because of their chemical diversity and complex matrices. In this work, a strategy combining high-resolution peak fractionation (HRPF) with a cell-based assay was proposed for target screening of bioactive constituents from natural products. In this approach, peak fractionation was conducted under chromatographic conditions optimized for high-resolution separation of the natural product extract. The HRPF approach was automatically performed according to the predefinition of certain peaks based on their retention times from a reference chromatographic profile. The corresponding HRPF database was collected with a parallel mass spectrometer to ensure purity and characterize the structures of compounds in the various fractions. Using this approach, a set of 75 peak fractions on the microgram scale was generated from 4mg of the extract of Salvia miltiorrhiza. After screening by an ARE-luciferase reporter gene assay, 20 diterpene quinones were selected and identified, and 16 of these compounds were reported to possess novel Nrf2 activation activity. Compared with conventional fixed-time interval fractionation, the HRPF approach could significantly improve the efficiency of bioactive compound discovery and facilitate the uncovering of minor active components. PMID:24406141

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

    PubMed

    Umamaheswari, Muthuswamy; Madeswaran, Arumugam; Asokkumar, Kuppusamy

    2013-01-01

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

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

    PubMed Central

    Umamaheswari, Muthuswamy; Madeswaran, Arumugam; Asokkumar, Kuppusamy

    2013-01-01

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

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

    NASA Astrophysics Data System (ADS)

    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.

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

    PubMed

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

    1996-07-01

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

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

    PubMed

    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. PMID:26724023

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

    SciTech Connect

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

    2015-12-15

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

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

    PubMed Central

    Fen, Li; Xuwei, Zhu; Nanyi, Li; Puyu, Zhang; Shuang, Zhang; Xue, Zhao; Pengju, Li; Qichao, Zhu; Haiping, Lin

    2014-01-01

    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. PMID:24693246

  15. Screening of lignocellulose-degrading superior mushroom strains and determination of their CMCase and laccase activity.

    PubMed

    Fen, Li; Xuwei, Zhu; Nanyi, Li; Puyu, Zhang; Shuang, Zhang; Xue, Zhao; Pengju, Li; Qichao, Zhu; Haiping, Lin

    2014-01-01

    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. PMID:24693246

  16. A genetic screen reveals a periplasmic copper chaperone required for nitrite reductase activity in pathogenic Neisseria.

    PubMed

    Jen, Freda E-C; Djoko, Karrera Y; Bent, Stephen J; Day, Christopher J; McEwan, Alastair G; Jennings, Michael P

    2015-09-01

    Under conditions of low oxygen availability, Neisseria meningitidis and Neisseria gonorrhoeae are able to respire via a partial denitrification pathway in which nitrite is converted to nitrous oxide. In this process, nitrite reductase (AniA), a copper (Cu)-containing protein converts nitrite to NO, and this product is converted to nitrous oxide by nitric oxide reductase (NorB). NorB also confers protection against toxic NO, and so we devised a conditional lethal screen, using a norB mutant, to identify mutants that were resistant to nitrite-dependent killing. After random-deletion mutagenesis of N. meningitidis, this genetic screen identified a gene encoding a Cu chaperone that is essential for AniA function, AccA. Purified AccA binds one Cu (I) ion and also possesses a second binding site for Cu (II). This novel periplasmic Cu chaperone (AccA) appears to be essential for provision of Cu ions to AniA of pathogenic Neisseria to generate an active nitrite reductase. Apart from the Neisseria genus, AccA is distributed across a wide range of environmental Proteobacteria species. PMID:26031293

  17. Microplate-based active/inactive 1° screen for biomass degrading enzyme library purification and gene discovery.

    PubMed

    Wagschal, Kurt; Lee, Charles C

    2012-04-01

    We present here a whole-cell and permeabilized E. coli cell 1° active/inactive microplate screen for β-d-xylosidase, xylanase, endoglucanase, and ferulic acid esterase enzyme activities, which are critical for the enzymatic deconstruction of biomass for fuels and chemicals. Transformants from genomic or mutagenesis-derived libraries are screened using fluorophore-tagged substrate/enzyme activity pairs that are assayed directly in the protein expression host growth media using a minimum of specialized equipment and supplies. PMID:22285853

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

    PubMed Central

    Bilsland, Elizabeth; Bean, Daniel M.; Devaney, Eileen; Oliver, Stephen G.

    2016-01-01

    Background 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. Methodology/Principal Findings 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. Conclusions/Significance 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

  19. Synthesis of Resveratrol Derivatives and In Vitro Screening for Potential Cancer Chemopreventive Activities.

    PubMed

    Orsini, Fulvia; Verotta, Luisella; Klimo, Karin; Gerhäuser, Clarissa

    2016-06-01

    New resveratrol (trans-3,4',5-trihydroxystilbene) analogs were synthesized and screened for their in vitro cancer chemopreventive potential using various bioassays relevant for the prevention of carcinogenesis in humans: two assays to detect modulators of carcinogen metabolism (Cyp1A inhibition; determination of NAD(P)H/quinone reductase (QR) activity), three assays to identify radical scavenging and antioxidant properties (DPPH, ORAC, superoxide anion radicals in differentiated HL-60 cells), four assays to determine anti-inflammatory and anti-hormonal effects (iNOS, Cox-1 and aromatase inhibition, anti-estrogenic potential). 3,4',5-Tri-O-methyl resveratrol 1a was about sevenfold more active than resveratrol in inhibiting Cyp1A activity, it was a potent inducer of QR activity, and it showed pure anti-estrogenic activity (whereas resveratrol is a known mixed estrogen (ant)agonist with both estrogenic and anti-estrogenic properties). Dual estrogen ant-/agonist activity was restored in the mono-O-benzyl-substituted derivatives 4b (4'-O-benzyl resveratrol) and 5b (3-O-benzyl resveratrol). With respect to aromatase inhibition (Cyp19), which provided the highest number of actives, the benzyl-substituted series was more potent than the methyl-substituted derivatives of resveratrol, and 3-O-benzyl resveratrol 5b was about eightfold more active than resveratrol. Overall, 3,4',5-tri-O-pivaloyl resveratrol oxide 7c was identified as a potent inducer of phase 2 enzymes concomitant with inhibition of LPS-mediated iNOS induction. PMID:27159630

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

    PubMed Central

    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

  1. Microplate-based active/inactive 1 screen for biomass degrading enzyme library purification and gene discovery

    Technology Transfer Automated Retrieval System (TEKTRAN)

    We present here a whole-cell and permeabilized E. coli cell 1' active/inactive microplate screen for ß-D-xylosidase, xylanase, endocellulase, and ferulic acid esterase enzyme activities which are critical for the enzymatic deconstruction of biomass for fuels and chemicals. Transformants from genomic...

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

    PubMed Central

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

    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 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. PMID:21772754

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

    PubMed

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

    2016-09-10

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

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

    PubMed Central

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

    2015-01-01

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

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

    PubMed

    Pessatti, M; Fontana, J D; Furtado, M F; Guimãraes, M F; Zanette, L R; Costa, W T; Baron, M

    1995-01-01

    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 of 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. PMID:7668847

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

    SciTech Connect

    Pessati, M.L.; Fontana, J.D.; Guimaraes, M.F.

    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.

  7. A high-content screening assay in transgenic zebrafish identifies two novel activators of fgf signaling.

    PubMed

    Saydmohammed, Manush; Vollmer, Laura L; Onuoha, Ezenwa Obi; Vogt, Andreas; Tsang, Michael

    2011-09-01

    Zebrafish have become an invaluable vertebrate animal model to interrogate small molecule libraries for modulators of complex biological pathways and phenotypes. We have recently described the implementation of a quantitative, high-content imaging assay in multi-well plates to analyze the effects of small molecules on Fibroblast Growth Factor (FGF) signaling in vivo. Here we have evaluated the capability of the assay to identify compounds that hyperactivate FGF signaling from a test cassette of agents with known biological activities. Using a transgenic zebrafish reporter line for FGF activity, we screened 1040 compounds from an annotated library of known bioactive agents, including FDA-approved drugs. The assay identified two molecules, 8-hydroxyquinoline sulfate and pyrithione zinc, that enhanced FGF signaling in specific areas of the brain. Subsequent studies revealed that both compounds specifically expanded FGF target gene expression. Furthermore, treatment of early stage embryos with either compound resulted in dorsalized phenotypes characteristic of hyperactivation of FGF signaling in early development. Documented activities for both agents included activation of extracellular signal-related kinase (ERK), consistent with FGF hyperactivation. To conclude, we demonstrate the power of automated quantitative high-content imaging to identify small molecule modulators of FGF. PMID:21932436

  8. Cholesterol oxidase with high catalytic activity from Pseudomonas aeruginosa: Screening, molecular genetic analysis, expression and characterization.

    PubMed

    Doukyu, Noriyuki; Nihei, Shyou

    2015-07-01

    An extracellular cholesterol oxidase producer, Pseudomonas aeruginosa strain PA157, was isolated by a screening method to detect 6β-hydroperoxycholest-4-en-3-one-forming cholesterol oxidase. On the basis of a putative cholesterol oxidase gene sequence in the genome sequence data of P. aeruginosa strain PAO1, the cholesterol oxidase gene from strain PA157 was cloned. The mature form of the enzyme was overexpressed in Escherichia coli cells. The overexpressed enzyme formed inclusion bodies in recombinant E. coli cells grown at 20 °C and 30 °C. A soluble and active PA157 enzyme was obtained when the recombinant cells were grown at 10 °C. The purified enzyme was stable at pH 5.5 to 10 and was most active at pH 7.5-8.0, showing optimal activity at pH 7.0 and 70 °C. The enzyme retained about 90% of its activity after incubation for 30 min at 70 °C. The enzyme oxidized 3β-hydroxysteroids such as cholesterol, β-cholestanol, and β-sitosterol at high rates. The Km value and Vmax value for the cholesterol were 92.6 μM and 15.9 μmol/min/mg of protein, respectively. The Vmax value of the enzyme was higher than those of commercially available cholesterol oxidases. This is the first report to characterize a cholesterol oxidase from P. aeruginosa. PMID:25573142

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

    PubMed

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

    2010-06-01

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

  10. How Young Children Spend Their Time: Television and Other Activities.

    ERIC Educational Resources Information Center

    Huston, Aletha C.; Wright, John C.; Marquis, Janet; Green, Samuel B.

    1999-01-01

    Examined television viewing over three years among two cohorts of 2- and 4-year olds. Found that viewing declined with age. With age, time in reading and educational activities increased on weekdays but declined on weekends, and sex differences in time-use patterns increased. Increased time in educational activities, social interaction, and video…

  11. Free Time Motivation and Physical Activity in Middle School Children

    ERIC Educational Resources Information Center

    Kozub, Francis M.; Farmer, James

    2011-01-01

    This study examined free time motivation and physical activity in 68 middle school children from a rural public school system (N = 24) and a private school located in the same area of the Midwest (N = 44). Results indicated that free time motivation did not explain variability in physical activity behavior during free time or while students were…

  12. Screening of free-living rhizospheric bacteria for their multiple plant growth promoting activities.

    PubMed

    Ahmad, Farah; Ahmad, Iqbal; Khan, M S

    2008-01-01

    Plant growth promoting rhizobacteria (PGPR) are known to influence plant growth by various direct or indirect mechanisms. In search of efficient PGPR strains with multiple activities, a total of 72 bacterial isolates belonging to Azotobacter, fluorescent Pseudomonas, Mesorhizobium and Bacillus were isolated from different rhizospheric soil and plant root nodules in the vicinity of Aligarh. These test isolates were biochemically characterized. These isolates were screened in vitro for their plant growth promoting traits like production of indoleacetic acid (IAA), ammonia (NH(3)), hydrogen cyanide (HCN), siderophore, phosphate solubilization and antifungal activity. More than 80% of the isolates of Azotobacter, fluorescent Pseudomonas and Mesorhizobium ciceri produced IAA, whereas only 20% of Bacillus isolates was IAA producer. Solubilization of phosphate was commonly detected in the isolates of Bacillus (80%) followed by Azotobacter (74.47%), Pseudomonas (55.56%) and Mesorhizobium (16.67%). All test isolates could produce ammonia but none of the isolates hydrolyzed chitin. Siderophore production and antifungal activity of these isolates except Mesorhizobium were exhibited by 10-12.77% isolates. HCN production was more common trait of Pseudomonas (88.89%) and Bacillus (50%). On the basis of multiple plant growth promoting activities, eleven bacterial isolates (seven Azotobacter, three Pseudomonas and one Bacillus) were evaluated for their quantitative IAA production, and broad-spectrum (active against three test fungi) antifungal activity. Almost at all concentration of tryptophan (50-500 microg/ml), IAA production was highest in the Pseudomonas followed by Azotobacter and Bacillus isolates. Azotobacter isolates (AZT(3), AZT(13), AZT(23)), Pseudomonas (Ps(5)) and Bacillus (B(1)) showed broad-spectrum antifungal activity on Muller-Hinton medium against Aspergillus, one or more species of Fusarium and Rhizoctonia bataticola. Further evaluation of the isolates

  13. Bioassay technique using nonspecific esterase activities of Tetrahymena pyriformis for screening and assessing cytotoxicity of xenobiotics

    SciTech Connect

    Bogaerts, P.; Senaud, J.; Bohatier, J. |

    1998-08-01

    A simple and rapid test for screening and assessing the cytotoxicity of xenobiotics was developed with Tetrahymena pyriformis. The method estimates the activities of nonspecific esterases of a cell by concentrating within it a specific amount of fluorescence associated with fluorescein dye. The 2-h median effective concentration (EC50) values of 10 inorganic and eight organic substances are presented and compared to those of three other bioassays: the conventional T. pyriformis proliferation rate 9-h median inhibitory concentrations, the Microtox 30-min EC50s, and the Daphnia magna 4-methylumbelliferyl {beta}-D galactoside 1-h EC50s. A highly significant correlation was found between the results obtained with the fluorescein diacetate test and those obtained with the growth inhibition and Microtox tests. This in vivo enzymatic test showed high sensitivity to all compounds tested except Cr{sup 6+} and sodium dodecyl sulfate.

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

    NASA Astrophysics Data System (ADS)

    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.

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

    PubMed

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

    2014-07-01

    In previous study, we have screened the effective fraction against Alzheimer's disease (AD-EF) from the extracts of roots and rhizomes of Valeriana amurensis, based on which neuroprotective active constituents from AD-EF were investigated. Six new compounds 1-6, including four iridoids (xiecaoside A-C and xiecaoline A), one pinane-type monoterpeneglucoside (xiecaoside D), and one phenylpropanoid glycoside (xiecaoside E) were isolated together with 11 known compounds 7-17. The structures of 1-6 were elucidated by their spectroscopic data. The protective effects of compounds 1-17 on PC12 cells with neurotoxicity induced by amyloid-beta 1-42 (Aβ(1-42)) was also investigated, respectively. Consequently, compound 6 and lignans 11-17 were responsible for protecting against Aβ-induced toxicity in PC12 cells. PMID:24742562

  16. Interrelationships of adolescent physical activity, screen-based sedentary behaviour, and social and psychological health

    PubMed Central

    Iannotti, Ronald J.; Janssen, Ian; Haug, Ellen; Kololo, Hanna; Annaheim, Beatrice; Borraccino, Alberto

    2009-01-01

    Summary Objectives To examine how adolescent physical activity (PA) and screen-based media sedentary behaviours (SBM) relate to psychological and social health and identify cross-national differences in these relationships. Methods Associations were examined in five regions using two Health Behaviour in School-Aged Children (HBSC) countries from each. Results Self-reported psychological and social health indices such as self-image, perceived health status, and quality of life were positively related to PA in all five regions but, with a few exceptions, negatively related to SBM. Negative health indices such as health complaints and tobacco use were negatively related to PA but, with exceptions, positively related to SBM. Significant regional differences were present. Conclusions Regional differences in correlates of PA and SBM suggest cultural differences in potential effects of PA and SBM and the need to tailor school and public health efforts to the different meanings of PA and SBM for positive and negative health consequences. PMID:19639256

  17. Surrogate screening models for the low physical activity criterion of frailty

    PubMed Central

    Eckel, Sandrah P.; Bandeen-Roche, Karen; Chaves, Paulo H.M.; Fried, Linda P.; Louis, Thomas A.

    2012-01-01

    Background and Aims Low physical activity, one of five criteria in a validated clinical phenotype of frailty, is assessed by a standardized, semi-quantitative questionnaire on up to 20 leisure time activities. Because of the time demanded to collect the interview data, it has been challenging to translate to studies other than the Cardiovascular Health Study (CHS), for which it was developed. Considering subsets of activities, we identified and evaluated streamlined surrogate assessment methods and compared them to one implemented in the Women’s Health and Aging Study (WHAS). Methods Using data on men and women ages 65 and older from the CHS, we applied logistic regression models to rank activities by “relative influence” in predicting low physical activity. We considered subsets of the most influential activities as inputs to potential surrogate models (logistic regressions). We evaluated predictive accuracy and predictive validity using the area under receiver operating characteristic curves and assessed criterion validity using proportional hazards models relating frailty status (defined using the surrogate) to mortality. Results Walking for exercise and moderately strenuous household chores were highly influential for both genders. Women required fewer activities than men for accurate classification. The WHAS model (8 CHS activities) was an effective surrogate, but a surrogate using 6 activities (walking, chores, gardening, general exercise, mowing and golfing) was also highly predictive. Conclusions We recommend a 6 activity questionnaire to assess physical activity for men and women. If efficiency is essential and the study involves only women, fewer activities can be included. PMID:21993168

  18. Informed Choice in the German Mammography Screening Program by Education and Migrant Status: Survey among First-Time Invitees.

    PubMed

    Berens, Eva-Maria; Reder, Maren; Razum, Oliver; Kolip, Petra; Spallek, Jacob

    2015-01-01

    Breast cancer is the most prevalent cancer among women and mammography screening programs are seen as a key strategy to reduce breast cancer mortality. In Germany, women are invited to the population-based mammography screening program between ages 50 to 69. It is still discussed whether the benefits of mammography screening outweigh its harms. Therefore, the concept of informed choice comprising knowledge, attitude and intention has gained importance. The objective of this observational study was to assess the proportion of informed choices among women invited to the German mammography screening program for the first time. A representative sample of 17,349 women aged 50 years from a sub-region of North Rhine Westphalia was invited to participate in a postal survey. Turkish immigrant women were oversampled. The effects of education level and migration status on informed choice and its components were assessed. 5,847 (33.7%) women responded to the postal questionnaire of which 4,113 were used for analyses. 31.5% of the women had sufficient knowledge. The proportion of sufficient knowledge was lower among immigrants and among women with low education levels. The proportion of women making informed choices was low (27.1%), with similar associations with education level and migration status. Women of low (OR 2.75; 95% CI 2.18-3.46) and medium education level (OR 1.49; 95% CI 1.27-1.75) were more likely to make an uninformed choice than women of high education level. Turkish immigrant women had the greatest odds for making an uninformed choice (OR 5.30, 95% CI 1.92-14.66) compared to non-immigrant women. Other immigrant women only had slightly greater odds for making an uninformed choice than non-immigrant women. As immigrant populations and women with low education level have been shown to have poor knowledge, they need special attention in measures to increase knowledge and thus informed choices. PMID:26529513

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

    PubMed Central

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

    2008-01-01

    Background Concerns have been raised about the biological and toxicologic effects of the antimicrobials triclocarban (TCC) and triclosan (TCS) in personal care products. Few studies have evaluated their biological activities in mammalian cells to assess their potential for adverse effects. Objectives In this study, we assessed the activity of TCC, its analogs, and TCS in in vitro nuclear-receptor–responsive and calcium signaling bioassays. Materials and methods We determined the biological activities of the compounds in in vitro, cell-based, and nuclear-receptor–responsive bioassays for receptors for aryl hydrocarbon (AhR), estrogen (ER), androgen (AR), and ryanodine (RyR1). Results Some carbanilide compounds, including TCC (1–10 μM), enhanced estradiol (E2)-dependent or testosterone-dependent activation of ER- and AR-responsive gene expression up to 2.5-fold but exhibited little or no agonistic activity alone. Some carbanilides and TCS exhibited weak agonistic and/or antagonistic activity in the AhR-responsive bioassay. TCS exhibited antagonistic activity in both ER- and AR-responsive bioassays. TCS (0.1–10 μM) significantly enhanced the binding of [3H]ryanodine to RyR1 and caused elevation of resting cytosolic [Ca2+] in primary skeletal myotubes, but carbanilides had no effect. Conclusions Carbanilides, including TCC, enhanced hormone-dependent induction of ER- and AR-dependent gene expression but had little agonist activity, suggesting a new mechanism of action of endocrine-disrupting compounds. TCS, structurally similar to noncoplanar ortho-substituted poly-chlorinated biphenyls, exhibited weak AhR activity but interacted with RyR1 and stimulated Ca2+ mobilization. These observations have potential implications for human and animal health. Further investigations are needed into the biological and toxicologic effects of TCC, its analogs, and TCS. PMID:18795164

  20. A high throughput drug screen based on fluorescence resonance energy transfer (FRET) for anticancer activity of compounds from herbal medicine

    PubMed Central

    Tian, H; Ip, L; Luo, H; Chang, D C; Luo, K Q

    2006-01-01

    Background and purpose: We report the development of a very efficient cell-based high throughput screening (HTS) method, which utilizes a novel bio-sensor that selectively detects apoptosis based on the fluorescence resonance energy transfer (FRET) technique. Experimental approach: We generated a stable HeLa cell line expressing a FRET-based bio-sensor protein. When cells undergo apoptosis, they activate a protease called ‘caspase-3'. Activation of this enzyme will cleave our sensor protein and cause its fluorescence emission to shift from a wavelength of 535 nm (green) to 486 nm (blue). A decrease in the green/blue emission ratio thus gives a direct indication of apoptosis. The sensor cells are grown in 96-well plates. After addition of different chemical compounds to each well, a fluorescence profile can be measured at various time-points using a fluorescent plate reader. Compounds that can trigger apoptosis are potential candidates as anti-cancer drugs. Key results: This novel cell-based HTS method is highly effective in identifying anti-cancer compounds. It was very sensitive in detecting apoptosis induced by various known anti-cancer drugs. Further, this system detects apoptosis, but not necrosis, and is thus more useful than the conventional cell viability assays, such as those using MTT. Finally, we used this system to screen compounds, isolated from two plants used in Chinese medicine, and identified several effective compounds for inducing apoptosis. Conclusions and Implications: This FRET-based HTS method is a powerful tool for identifying anti-cancer compounds and can serve as a highly efficient platform for drug discovery. PMID:17179946

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

    PubMed

    Kumar, Vijay; Bharti, Alpana; Negi, Yogesh Kumar; Gusain, Omprakash; Pandey, Piyush; Bisht, Gajraj Singh

    2012-01-01

    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. PMID:24031819

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

    PubMed

    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. PMID:25714885

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

    PubMed Central

    Kumar, Vijay; Bharti, Alpana; Negi, Yogesh Kumar; Gusain, Omprakash; Pandey, Piyush; Bisht, Gajraj Singh

    2012-01-01

    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. PMID:24031819

  4. Rapid screening and quantitative determination of bioactive compounds from fruit extracts of Myristica species and their in vitro antiproliferative activity.

    PubMed

    Pandey, Renu; Mahar, Rohit; Hasanain, Mohammad; Shukla, Sanjeev K; Sarkar, Jayanta; Rameshkumar, K B; Kumar, Brijesh

    2016-11-15

    Efficient and sensitive LC-MS/MS methods have been developed for the rapid screening and determination of bioactive compounds in different fruit parts of four Myristica species, viz., Myristica beddomeii, Myristica fragrans, Myristica fatua and Myristica malabarica. Twenty-one compounds were identified and characterized on the basis of their accurate mass and MS/MS fragmentation pattern using HPLC-QTOF-MS/MS and NMR analysis. Quantitative determination of five major bioactive compounds was performed using multiple-reaction monitoring mode with continuous polarity switching by UHPLC-QqQLIT-MS/MS. Moreover, in vitro antiproliferative activity of these Myristica species was evaluated against five human cancer cell lines A549, DLD-1, DU145, FaDu and MCF-7 using SRB assay. Seventeen phytoconstituents were identified and reported for the first time from M. beddomeii and sixteen from M. fatua. Quantification result showed highest total content of five major bioactive compounds in mace of M. fragrans. Evaluation of in vitro antiproliferative activity revealed potent activity in all investigated species except M. fragrans. PMID:27283658

  5. Unbiased identification of signal-activated transcription factors by barcoded synthetic tandem repeat promoter screening (BC-STAR-PROM).

    PubMed

    Gosselin, Pauline; Rando, Gianpaolo; Fleury-Olela, Fabienne; Schibler, Ueli

    2016-08-15

    The discovery of transcription factors (TFs) controlling pathways in health and disease is of paramount interest. We designed a widely applicable method, dubbed barcorded synthetic tandem repeat promoter screening (BC-STAR-PROM), to identify signal-activated TFs without any a priori knowledge about their properties. The BC-STAR-PROM library consists of ∼3000 luciferase expression vectors, each harboring a promoter (composed of six tandem repeats of synthetic random DNA) and an associated barcode of 20 base pairs (bp) within the 3' untranslated mRNA region. Together, the promoter sequences encompass >400,000 bp of random DNA, a sequence complexity sufficient to capture most TFs. Cells transfected with the library are exposed to a signal, and the mRNAs that it encodes are counted by next-generation sequencing of the barcodes. This allows the simultaneous activity tracking of each of the ∼3000 synthetic promoters in a single experiment. Here we establish proof of concept for BC-STAR-PROM by applying it to the identification of TFs induced by drugs affecting actin and tubulin cytoskeleton dynamics. BC-STAR-PROM revealed that serum response factor (SRF) is the only immediate early TF induced by both actin polymerization and microtubule depolymerization. Such changes in cytoskeleton dynamics are known to occur during the cell division cycle, and real-time bioluminescence microscopy indeed revealed cell-autonomous SRF-myocardin-related TF (MRTF) activity bouts in proliferating cells. PMID:27601530

  6. Interlaboratory validation of quantitative duplex real-time PCR method for screening analysis of genetically modified maize.

    PubMed

    Takabatake, Reona; Koiwa, Tomohiro; Kasahara, Masaki; Takashima, Kaori; Futo, Satoshi; Minegishi, Yasutaka; Akiyama, Hiroshi; Teshima, Reiko; Oguchi, Taichi; Mano, Junichi; Furui, Satoshi; Kitta, Kazumi

    2011-01-01

    To reduce the cost and time required to routinely perform the genetically modified organism (GMO) test, we developed a duplex quantitative real-time PCR method for a screening analysis simultaneously targeting an event-specific segment for GA21 and Cauliflower Mosaic Virus 35S promoter (P35S) segment [Oguchi et al., J. Food Hyg. Soc. Japan, 50, 117-125 (2009)]. To confirm the validity of the method, an interlaboratory collaborative study was conducted. In the collaborative study, conversion factors (Cfs), which are required to calculate the GMO amount (%), were first determined for two real-time PCR instruments, the ABI PRISM 7900HT and the ABI PRISM 7500. A blind test was then conducted. The limit of quantitation for both GA21 and P35S was estimated to be 0.5% or less. The trueness and precision were evaluated as the bias and reproducibility of the relative standard deviation (RSD(R)). The determined bias and RSD(R) were each less than 25%. We believe the developed method would be useful for the practical screening analysis of GM maize. PMID:21873818

  7. [Simple and rapid screening for psychotropic natural products using Direct Analysis in Real Time (DART)-TOFMS].

    PubMed

    Kawamura, Maiko; Kikura-Hanajiri, Ruri; Goda, Yukihiro

    2009-06-01

    Direct Analysis in Real Time (DART) is a novel ionization technique that provides for the rapid ionization of small molecules under ambient conditions. To investigate the trend of non-controlled psychotropic plants of abuse in Japan, a rapid screening method, without sample preparation, was developed using DART-time of flight mass spectrometer (TOFMS) for plant products. The major psychotropic constituents of these products were determined using liquid chromatography-mass spectrometry (LC/MS). As a result of the DART-TOFMS analyses of 36 products, the protonated molecular ions [M+H](+), corresponding to 6 kinds of major hallucinogenic constituents (mescaline, salvinorin A, N,N-dimethyltryptamine, harmine, harmaline and lysergamide), were detected in 21 products. It was possible to estimate their accurate elemental compositions through exact mass measurements. These results were consistent with those of the LC/MS analyses and the contents of the 6 psychotropic constituents were in the range from 0.05 to 45 microg/mg. Typical controlled narcotic drugs, tetrahydrocannabinol, opioid alkaloids and psilocin were also directly detected in marijuana cigarette, opium gum and magic mushroom respectively. Although it is difficult to estimate the matrix effects caused by other plant ingredients, the DART-TOFMS could be useful as a simple and rapid screening method for the targeted psychotropic natural products, because it provides the molecular information of the target compounds without time-consuming extraction and pre-treatment steps. PMID:19483414

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

    PubMed

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

    2013-04-01

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

  9. Screening for hetero-transglycosylating activities in extracts from nasturtium (Tropaeolum majus).

    PubMed

    Mohand, Fairouz Ait; Farkas, Vladimír

    2006-04-10

    Using combinations of different polysaccharides as glycosyl donors and of oligosaccharides fluorescently labeled by sulforhodamine (SR) as glycosyl acceptors, we screened for the presence of transglycosylating activities in extracts from nasturtium (Tropaeolum majus). Besides xyloglucan endotransglycosylase/hydrolase (XTH/XET, EC 2.4.1.207) activity, which transfers xyloglucanosyl residues from xyloglucan (XG) to XG-derived oligosaccharides (XGOs), a glycosyl transfer from XG to SR-labeled cellooligosaccharides and laminarioligosaccharides has been detected. The XGOs also served as acceptors for the glycosyl transfer from soluble cellulose derivatives carboxymethyl cellulose and hydroxyethylcellulose. The effectivity of these polysaccharides as glycosyl donors for transfer to XG-derived octasaccharide [1-3H]XXLGol decreased in the order XG > HEC > CMC. Isoelectric focusing in polyacrylamide gels showed that bands corresponding to hetero-transglycosylase activities coincided with zones corresponding to XTH/XET. These results can be explained as due either to substrate non-specificity of certain isoenzymes of XTH/XET or to existence of enzymes catalyzing a hetero-transfer, that is the formation of covalent linkages between different types of carbohydrate polymers. PMID:16445892

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

    PubMed Central

    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

  11. Assessment of estrogenic activity in Tunisian water and wastewater by E-screen assay.

    PubMed

    Limam, Atef; Talorete, Terence P N; Ali, Mourad Ben Sik; Kawano, Mitsuko; Jenhani, Amel Ben Rejeb; Abe, Yukuo; Ghrabi, Ahmed; Isoda, Hiroko

    2007-01-01

    Wastewater and surface water samples from three wastewater treatment plants (WWTPs) and three rivers in Tunisia were assayed for estrogenic activity using the E-screen assay and enzyme-linked immunosorbent assay (ELISA). Results showed that all the Tunisian raw wastewater samples as well as the Roriche river water sample induced a strong proliferative response in human MCF-7 breast cancer cells. Tunisian raw wastewater had an average 17beta-estradiol content of 2,705.4 pg/ml, whereas that of the Roriche river was 36.7 pg/ml, which is sufficient for inducing endocrine-mediated responses in aquatic organisms. Results further showed that the Mornag WWTP, which uses the activated-sludge treatment system, has a higher estrogen removal efficiency than the stabilization ponds of the Gammart and pilot WWTPs. This study, which is the first of such studies in Tunisia, and probably the first in the North African region, underscores the need to detect and monitor the estrogenic activity of water and wastewater, given the scarcity of water in Tunisia and the detrimental impact of endocrine-disrupting compounds on the physiology of both animals and humans. PMID:18382414

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

    PubMed Central

    2012-01-01

    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. PMID:22963538

  13. Enzyme family-specific and activity-based screening of chemical libraries using enzyme microarrays.

    PubMed

    Funeriu, Daniel P; Eppinger, Jörg; Denizot, Lucile; Miyake, Masato; Miyake, Jun

    2005-05-01

    The potential of protein microarrays in high-throughput screening (HTS) still remains largely unfulfilled, essentially because of the difficulty of extracting meaningful, quantitative data from such experiments. In the particular case of enzyme microarrays, low-molecular-weight fluorescent affinity labels (FALs) can function as ideally suited activity probes of the microarrayed enzymes. FALs form covalent bonds with enzymes in an activity-dependent manner and therefore can be used to characterize enzyme activity at each enzyme's address, as predetermined by the microarraying process. Relying on this principle, we introduce herein thematic enzyme microarrays (TEMA). In a kinetic setup we used TEMAs to determine the full set of kinetic constants and the reaction mechanism between the microarrayed enzymes (the theme of the microarray) and a family-wide FAL. Based on this kinetic understanding, in an HTS setup we established the practical and theoretical methodology for quantitative, multiplexed determination of the inhibition profile of compounds from a chemical library against each microarrayed enzyme. Finally, in a validation setup, K(i)(app) values and inhibitor profiles were confirmed and refined. PMID:15821728

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

    PubMed Central

    2012-01-01

    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. PMID:22640773

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

    PubMed

    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 <1000 mg L(-1)) in the brine shrimp bioassay. For 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. PMID:18075897

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

    PubMed

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

    2011-11-28

    The three-dimensional (3D) structures of most protein targets have not been determined so far, with many of them not even having a known ligand, a truly general method to predict ligand-protein interactions in the absence of three-dimensional information would be of great potential value in drug discovery. Using the support vector machine (SVM) approach, we constructed a model for predicting ligand-protein interaction based only on the primary sequence of proteins and the structural features of small molecules. The model, trained by using 15,000 ligand-protein interactions between 626 proteins and over 10,000 active compounds, was successfully used in discovering nine novel active compounds for four pharmacologically important targets (i.e., GPR40, SIRT1, p38, and GSK-3β). To our knowledge, this is the first example of a successful sequence-based virtual screening campaign, demonstrating that our approach has the potential to discover, with a single model, active ligands for any protein. PMID:21955088

  17. Cell-Based Screening Identifies the Active Ingredients from Traditional Chinese Medicine Formula Shixiao San as the Inhibitors of Atherosclerotic Endothelial Dysfunction

    PubMed Central

    Wang, Xiaofan; Zhang, Ruowen; Gu, Liqiang; Zhang, Yuanyuan; Zhao, Xu; Bi, Kaishun; Chen, Xiaohui

    2015-01-01

    In this study, we performed a phenotypic screening in human endothelial cells exposed to oxidized low density lipoprotein (an in vitro model of atherosclerotic endothelial dysfunction) to identify the effective compounds in Shixiao San. After investigating the suitability and reliability of the cell-based screening method using atorvastatin as the positive control drug, this method was applied in screening Shixiao San and its extracts. The treatment of n-butanol fraction on endothelial cells exhibited stronger healing effects against oxidized low density lipoprotein-induced insult when compared with other fractions. Cell viability, the level of nitric oxide, endothelial nitric oxide synthase and endothelin-1 were measured, respectively. The assays revealed n-butanol fraction significantly elevated the survival ratio of impaired cells in culture. In parallel, n-butanol fraction exhibited the highest inhibition of inflammation. The generation of prostaglandin-2 and adhesion molecule (soluble intercellular adhesion molecule-1) was obviously declined. Furthermore, n-butanol fraction suppressed the production of reactive oxygen species and malondialdehyde, and restored the activity of superoxide dismutase. Compounds identification of the n-butanol fraction was carried out by ultra high liquid chromatography coupled to quadrupole time-of-flight tandem mass spectrometry. The active ingredients including quercetin-3-O-(2G-α-l-rhamnosyl)-rutinoside, quercetin-3-O-neohesperidoside, isorhamnetin-3-O-neohesperidoside and isorhamnetin-3-O-rutinoside revealed the ability of anti-atherosclerosis after exposing on endothelial cells. The current work illustrated the pharmacology effect of Shixiao San and clearly indicated the major active components in Shixiao San. More importantly, the proposed cell-based screening method might be particularly suitable for fast evaluating the anti-atherosclerosis efficacy of Traditional Chinese Medicines and screening out the interesting

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

    PubMed Central

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

    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, 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 2 000 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. PMID:23570014

  19. In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen

    PubMed Central

    Plouffe, David; Brinker, Achim; McNamara, Case; Henson, Kerstin; Kato, Nobutaka; Kuhen, Kelli; Nagle, Advait; Adrián, Francisco; Matzen, Jason T.; Anderson, Paul; Nam, Tae-gyu; Gray, Nathanael S.; Chatterjee, Arnab; Janes, Jeff; Yan, S. Frank; Trager, Richard; Caldwell, Jeremy S.; Schultz, Peter G.; Zhou, Yingyao; Winzeler, Elizabeth A.

    2008-01-01

    The growing resistance to current first-line antimalarial drugs represents a major health challenge. To facilitate the discovery of new antimalarials, we have implemented an efficient and robust high-throughput cell-based screen (1,536-well format) based on proliferation of Plasmodium falciparum (Pf) in erythrocytes. From a screen of ≈1.7 million compounds, we identified a diverse collection of ≈6,000 small molecules comprised of >530 distinct scaffolds, all of which show potent antimalarial activity (<1.25 μM). Most known antimalarials were identified in this screen, thus validating our approach. In addition, we identified many novel chemical scaffolds, which likely act through both known and novel pathways. We further show that in some cases the mechanism of action of these antimalarials can be determined by in silico compound activity profiling. This method uses large datasets from unrelated cellular and biochemical screens and the guilt-by-association principle to predict which cellular pathway and/or protein target is being inhibited by select compounds. In addition, the screening method has the potential to provide the malaria community with many new starting points for the development of biological probes and drugs with novel antiparasitic activities. PMID:18579783

  20. Time to pay attention: attentional performance time-stamped prefrontal cholinergic activation, diurnality and performance

    PubMed Central

    Paolone, Giovanna; Lee, Theresa M.; Sarter, Martin

    2012-01-01

    Although the impairments in cognitive performance that result from shifting or disrupting daily rhythms have been demonstrated, the neuronal mechanisms that optimize fixed time daily performance are poorly understood. We previously demonstrated that daily practice of a sustained attention task (SAT) evokes a diurnal activity pattern in rats. Here we report that SAT practice at a fixed time produced practice time-stamped increases in prefrontal cholinergic neurotransmission that persisted after SAT practice was terminated and in a different environment. SAT time-stamped cholinergic activation occurred irrespective of whether the SAT was practiced during the light or dark phase or in constant light conditions. In contrast, prior daily practice of an operant schedule of reinforcement, albeit generating more rewards and lever presses per session than the SAT, neither activated the cholinergic system nor affected the animals' nocturnal activity pattern. Likewise, food-restricted animals exhibited strong food anticipatory activity (FAA) and attenuated activity during the dark period but FAA was not associated with increases in prefrontal cholinergic activity. Removal of cholinergic neurons impaired SAT performance and facilitated the reemergence of nocturnality. Shifting SAT practice away from a fixed time resulted in significantly lower performance. In conclusion, these experiments demonstrated that fixed time, daily practice of a task assessing attention generates a precisely practice time-stamped activation of the cortical cholinergic input system. Time-stamped cholinergic activation benefits fixed time performance and, if practiced during the light phase, contributes to a diurnal activity pattern. PMID:22933795

  1. Identification of Thyroid Hormone Receptor Active Compounds Using a Quantitative High-Throughput Screening Platform

    PubMed Central

    Freitas, Jaime; Miller, Nicole; Mengeling, Brenda J.; Xia, Menghang; Huang, Ruili; Houck, Keith; Rietjens, Ivonne M.C.M.; Furlow, J. David; Murk, Albertinka J.

    2014-01-01

    To adapt the use of GH3.TRE-Luc reporter gene cell line for a quantitative high-throughput screening (qHTS) platform, we miniaturized the reporter gene assay to a 1536-well plate format. 1280 chemicals from the Library of Pharmacologically Active Compounds (LOPAC) and the National Toxicology Program (NTP) 1408 compound collection were analyzed to identify potential thyroid hormone receptor (TR) agonists and antagonists. Of the 2688 compounds tested, eight scored as potential TR agonists when the positive hit cut-off was defined at ≥10% efficacy, relative to maximal triiodothyronine (T3) induction, and with only one of those compounds reaching ≥20% efficacy. One common class of compounds positive in the agonist assays were retinoids such as all-trans retinoic acid, which are likely acting via the retinoid-X receptor, the heterodimer partner with the TR. Five potential TR antagonists were identified, including the antiallergy drug tranilast and the anxiolytic drug SB 205384 but also some cytotoxic compounds like 5-fluorouracil. None of the inactive compounds were structurally related to T3, nor had been reported elsewhere to be thyroid hormone disruptors, so false negatives were not detected. None of the low potency (>100µM) TR agonists resembled T3 or T4, thus these may not bind directly in the ligand-binding pocket of the receptor. For TR agonists, in the qHTS, a hit cut-off of ≥20% efficacy at 100 µM may avoid identification of positives with low or no physiological relevance. The miniaturized GH3.TRE-Luc assay offers a promising addition to the in vitro test battery for endocrine disruption, and given the low percentage of compounds testing positive, its high-throughput nature is an important advantage for future toxicological screening. PMID:24772387

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

    PubMed Central

    2013-01-01

    Background The development of resistance to chemotherapies represents a significant barrier to successful cancer treatment. Resistance mechanisms are complex, can involve diverse and often unexpected cellular processes, and can vary with both the underlying genetic lesion and the origin or type of tumor. For these reasons developing experimental strategies that could be used to understand, identify and predict mechanisms of resistance in different malignant cells would be a major advance. Methods Here we describe a gain-of-function forward genetic approach for identifying mechanisms of resistance. This approach uses a modified piggyBac transposon to generate libraries of mutagenized cells, each containing transposon insertions that randomly activate nearby gene expression. Genes of interest are identified using next-gen high-throughput sequencing and barcode multiplexing is used to reduce experimental cost. Results Using this approach we successfully identify genes involved in paclitaxel resistance in a variety of cancer cell lines, including the multidrug transporter ABCB1, a previously identified major paclitaxel resistance gene. Analysis of co-occurring transposons integration sites in single cell clone allows for the identification of genes that might act cooperatively to produce drug resistance a level of information not accessible using RNAi or ORF expression screening approaches. Conclusion We have developed a powerful pipeline to systematically discover drug resistance in mammalian cells in vitro. This cost-effective approach can be readily applied to different cell lines, to identify canonical or context specific resistance mechanisms. Its ability to probe complex genetic context and non-coding genomic elements as well as cooperative resistance events makes it a good complement to RNAi or ORF expression based screens. PMID:23442791

  3. Miniaturizable homogenous time-resolved fluorescence assay for carboxypeptidase B activity.

    PubMed

    Ferrer, Marc; Zuck, Paul; Kolodin, Garrett; Mao, Shi Shan; Peltier, Richard R; Bailey, Carolyn; Gardell, Stephen J; Strulovici, Berta; Inglese, James

    2003-06-01

    An epitope-unmasking, homogeneous time-resolved fluorescence (HTRF) assay has been developed for measuring carboxypeptidase B (CPB) activity in a miniaturized high-throughput screening format. The enzyme substrate (biotin-RYRGLMVGGVVR-OH) is cleaved by CPB at the C terminus, causing release of the C-terminal Arg residue. The product (biotin-RYRGLMVGGVV-OH) is recognized specifically by a monoclonal antibody (G2-10) which is labeled with Eu(3+)-cryptate ([Eu(3+)]G2-10 mAb), and the complex is detected by fluorescence resonance energy transfer using streptavidin labeled with allophycocyanin ([XL665]SA). The CPB HTRF assay is readily adapted from 96- to 1536-well format as a robust (Z(')>0.5) assay for high-throughput screening. PMID:12729605

  4. The better the story, the bigger the serving: narrative transportation increases snacking during screen time in a randomized trial

    PubMed Central

    2013-01-01

    Background Watching television and playing video games increase energy intake, likely due to distraction from satiety cues. A study comparing one hour of watching TV, playing typical video games, or playing motion-controlled video games found a difference across groups in energy intake, but the reasons for this difference are not clear. As a secondary analysis, we investigated several types of distraction to determine potential psychosocial mechanisms which may account for greater energy intake observed during sedentary screen time as compared to motion-controlled video gaming. Methods Feelings of enjoyment, engagement (mental immersion), spatial presence (the feeling of being in the game), and transportation (immersion in a narrative) were investigated in 120 young adults aged 18 – 35 (60 female). Results Only narrative transportation was associated with total caloric intake (ρ = .205, P = .025). Transportation was also higher in the TV group than in the gaming groups (P = .002) and higher in males than in females (P = .003). Transportation mediated the relationship between motion-controlled gaming (as compared to TV watching) and square root transformed energy intake (indirect effect = −1.34, 95% confidence interval −3.57, −0.13). No other distraction-related variables were associated with intake. Conclusions These results suggest that different forms of distraction may differentially affect eating behavior during screen time, and that narrative appears to be a particularly strong distractor. Future studies should further investigate the effects of narrative on eating behavior. PMID:23680389

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

    PubMed Central

    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

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

    PubMed Central

    Nikolova, Milena

    2011-01-01

    Background: Discovery of new plant species with antioxidant properties is a priority of many research teams. Most of the species included in this study are unstudied for antioxidant properties, but they are taxonomically related to reference plants with well-documented antioxidant activity. Materials and Methods: Free radical scavenging activity of plant extracts was evaluated using a 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. An aluminum chloride colorimetric method was used for flavonoid 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., Stachysrecta 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. PMID:22224049

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

    PubMed Central

    2010-01-01

    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. PMID:20470421

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

    PubMed

    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

  9. Screening of traditional Chinese medicinal plants for quorum-sensing inhibitors activity.

    PubMed

    Koh, Khee Hoon; Tham, Foong-Yee

    2011-04-01

    The misuse of antibiotics has contributed to widespread development of antimicrobial resistance among clinically significant bacterial species. Alternative approaches other than those using antibiotics are needed in the fight against infectious diseases. Quorum sensing (QS) is an intercellular signaling and gene regulatory mechanism, which is used by a number of opportunistic pathogenic bacteria in determining virulence gene expression. The study of QS may yield another strategy for disease control by interference with QS signals. Scientific research on complementary therapies such as traditional Chinese medicine (TCM) has focused mainly on its antibacterial properties. To test for anti-QS activity, 10 TCM herbs were screened using two biomonitor strains, Chromobacterium violaceum CV026 and Pseudomonas aeruginosa PA01. Interference with violacein (purple pigment) production in CV026 (exogenously supplied with homoserine lactone signals), and swarming in PA01, both QS-regulated phenomena, was used as indication of anti-QS activity. Eight of the selected TCM (80%) yielded QS inhibitors: Prunus armeniaca, Prunella vulgaris, Nelumbo nucifera, Panax notoginseng (root and flower), Punica granatum, Areca catechu, and Imperata cylindrica. Compounds that interfere with QS are present in TCM herbs and these medicines may be a rich source of compounds to combat pathogenic bacteria and reduce the development of antibiotic resistance. PMID:21439518

  10. Perspective: Web-based machine learning models for real-time screening of thermoelectric materials properties

    NASA Astrophysics Data System (ADS)

    Gaultois, Michael W.; Oliynyk, Anton O.; Mar, Arthur; Sparks, Taylor D.; Mulholland, Gregory J.; Meredig, Bryce

    2016-05-01

    The experimental search for new thermoelectric materials remains largely confined to a limited set of successful chemical and structural families, such as chalcogenides, skutterudites, and Zintl phases. In principle, computational tools such as density functional theory (DFT) offer the possibility of rationally guiding experimental synthesis efforts toward very different chemistries. However, in practice, predicting thermoelectric properties from first principles remains a challenging endeavor [J. Carrete et al., Phys. Rev. X 4, 011019 (2014)], and experimental researchers generally do not directly use computation to drive their own synthesis efforts. To bridge this practical gap between experimental needs and computational tools, we report an open machine learning-based recommendation engine (http://thermoelectrics.citrination.com) for materials researchers that suggests promising new thermoelectric compositions based on pre-screening about 25 000 known materials and also evaluates the feasibility of user-designed compounds. We show this engine can identify interesting chemistries very different from known thermoelectrics. Specifically, we describe the experimental characterization of one example set of compounds derived from our engine, RE12Co5Bi (RE = Gd, Er), which exhibits surprising thermoelectric performance given its unprecedentedly high loading with metallic d and f block elements and warrants further investigation as a new thermoelectric material platform. We show that our engine predicts this family of materials to have low thermal and high electrical conductivities, but modest Seebeck coefficient, all of which are confirmed experimentally. We note that the engine also predicts materials that may simultaneously optimize all three properties entering into zT; we selected RE12Co5Bi for this study due to its interesting chemical composition and known facile synthesis.

  11. Real-time spectroscopic monitoring of photocatalytic activity promoted by graphene in a microfluidic reactor.

    PubMed

    Li, Yifan; Lin, Beichen; Ge, Likai; Guo, Hongchen; Chen, Xinyi; Lu, Miao

    2016-01-01

    Photocatalytic microreactors have been utilized as rapid, versatile platforms for the characterization of photocatalysts. In this work, a photocatalytic microreactor integrated with absorption spectroscopy was proposed for the real-time monitoring of photocatalytic activity using different catalysts. The validity of this method was investigated by the rapid screening on the photocatalytic performance of a titanium oxide (TiO2)-decorated graphene oxide (GO) sheet for the degradation of methylene blue under monochromatic visible irradiation. The sampling interval time could be minimized to 10 s for achieving real-time detection. The best photocatalytic activity was observed for an optimized TiO2/GO weight mixing ratio of 7:11, with a reaction rate constant up to 0.067 min(-1). The addition of GO into TiO2 enhances photocatalytic activity and adsorption of MB molecules. The synthetic reaction rate constant was up to approximately 0.11 min(-1), which was also the highest among the catalysts. The microreactor exhibited good sensitivity and reproducibility without weakening the performance of the photocatalysts. Consequently, the photocatalytic microreactor is promising as a simple, portable, and rapid screening tool for new photocatalysts. PMID:27346555

  12. Real-time spectroscopic monitoring of photocatalytic activity promoted by graphene in a microfluidic reactor

    PubMed Central

    Li, Yifan; Lin, Beichen; Ge, Likai; Guo, Hongchen; Chen, Xinyi; Lu, Miao

    2016-01-01

    Photocatalytic microreactors have been utilized as rapid, versatile platforms for the characterization of photocatalysts. In this work, a photocatalytic microreactor integrated with absorption spectroscopy was proposed for the real-time monitoring of photocatalytic activity using different catalysts. The validity of this method was investigated by the rapid screening on the photocatalytic performance of a titanium oxide (TiO2)-decorated graphene oxide (GO) sheet for the degradation of methylene blue under monochromatic visible irradiation. The sampling interval time could be minimized to 10 s for achieving real-time detection. The best photocatalytic activity was observed for an optimized TiO2/GO weight mixing ratio of 7:11, with a reaction rate constant up to 0.067 min−1. The addition of GO into TiO2 enhances photocatalytic activity and adsorption of MB molecules. The synthetic reaction rate constant was up to approximately 0.11 min−1, which was also the highest among the catalysts. The microreactor exhibited good sensitivity and reproducibility without weakening the performance of the photocatalysts. Consequently, the photocatalytic microreactor is promising as a simple, portable, and rapid screening tool for new photocatalysts. PMID:27346555

  13. Real-time spectroscopic monitoring of photocatalytic activity promoted by graphene in a microfluidic reactor

    NASA Astrophysics Data System (ADS)

    Li, Yifan; Lin, Beichen; Ge, Likai; Guo, Hongchen; Chen, Xinyi; Lu, Miao

    2016-06-01

    Photocatalytic microreactors have been utilized as rapid, versatile platforms for the characterization of photocatalysts. In this work, a photocatalytic microreactor integrated with absorption spectroscopy was proposed for the real-time monitoring of photocatalytic activity using different catalysts. The validity of this method was investigated by the rapid screening on the photocatalytic performance of a titanium oxide (TiO2)-decorated graphene oxide (GO) sheet for the degradation of methylene blue under monochromatic visible irradiation. The sampling interval time could be minimized to 10 s for achieving real-time detection. The best photocatalytic activity was observed for an optimized TiO2/GO weight mixing ratio of 7:11, with a reaction rate constant up to 0.067 min‑1. The addition of GO into TiO2 enhances photocatalytic activity and adsorption of MB molecules. The synthetic reaction rate constant was up to approximately 0.11 min‑1, which was also the highest among the catalysts. The microreactor exhibited good sensitivity and reproducibility without weakening the performance of the photocatalysts. Consequently, the photocatalytic microreactor is promising as a simple, portable, and rapid screening tool for new photocatalysts.

  14. System, device, and methods for real-time screening of live cells, biomarkers, and chemical signatures

    DOEpatents

    Sundaram, S Kamakshi [Richland, WA; Riley, Brian J [West Richland, WA; Weber, Thomas J [Richland, WA; Sacksteder, Colette A [West Richland, WA; Addleman, R Shane [Benton City, WA

    2011-06-07

    An ATR-FTIR device and system are described that defect live-cell responses to stimuli and perturbations in real-time. The system and device can monitor perturbations resulting from exposures to various physical, chemical, and biological materials in real-time, as well as those sustained over a long period of time, including those associated with stimuli having unknown modes-of-action (e.g. nanoparticles). The device and system can also be used to identify specific chemical species or substances that profile cellular responses to these perturbations.

  15. Potential for health screening using long-term cardiovascular parameters measured by finger volume-oscillometry: pilot comparative evaluation in regular and sleep-deprived activities.

    PubMed

    Yamakoshi, Takehiro; Matsumura, Kenta; Rolfe, Peter; Hanaki, Shota; Ikarashi, Akira; Lee, Jihyoung; Yamakoshi, Ken-Ichi

    2014-01-01

    We explored the potential of health screening based on the long-term measurement of cardiovascular parameters using the finger volume-oscillometric technique. An automated instrument made simultaneous measurements of key cardiovascular parameters, including blood pressure, pulse pressure, heart rate, normalized pulse volume as an index of α-adrenalin-mediated sympathetic activity, and finger arterial elasticity. These were derived from finger photo-plethysmographic signals during application of cuff pressure. To assess the feasibility of achieving a screening function, measurements were made in ten healthy volunteers during 10 days of day-to-day living (normal condition), and carried out several times at a fixed time every day. During successive 10-day measurements, a 30-hour period of total sleep deprivation was introduced as a physiological challenge (abnormal condition). A linear discriminant analysis of the data was conducted to determine whether these two conditions could be discriminated. Periodic data collection was performed rapidly and easily, and the %-correct classifications of normal and abnormal conditions were 78.2% and 77.5%, respectively. This ability of the method to discriminate between regular and sleep-deprived activities demonstrates its potential for healthcare screening during day-to-day living. Further investigations using larger age and gender groups of subjects including patients with cardiovascular diseases under real-life situations are required. PMID:24403401

  16. [Enterobacter agglomerans B1 producing beta-galactosidase with transglycosylation activity: screening, identification, fermentation conditions, and galacto-oligosaccharides synthesis].

    PubMed

    Lu, Lili; Xiao, Min; Xu, Xiaodong

    2008-01-01

    Galacto-oligosaccharides (GOS) are promising non-digestible oligosaccharides recognized as prebiotics. Commercial GOS containing galactose as subunit, are synthesized from lactose using the galactosyl-transferase activity of beta-galactosidase. A strain producing beta-galactosidase with transglycosylation activity was screened from the soil. Phenotypic analysis including morphology and physiology characteristics and 16S rDNA sequence analysis were carried out. Based on taxonomy results, the strain was identified as Enterobacter agglomerans B1. Medium and fermentation conditions were optimized by single factor and orthogonal experiments. The enzyme reached 9.7 U/mL in the medium (pH 7.5) containing 1% lactose, 1% yeast extract, and 0.5% peptone when cultured at 25 degrees C for 26 h. Effects of pH, temperature, lactose concentration, and reaction time on transgalactosylation by whole cells were studied. Yield of GOS reached 40.7% in 30% lactose (pH 7.5) at 50 degrees C for 12 h, as analyzed by HPLC and TLC. The results of an MS analysis showed that GOS were composed of di, tri-, and tetrasaccharides. PMID:18338574

  17. Screening for hemostatic activities of popular Chinese medicinal herbs in vitro

    PubMed Central

    Ohkura, Naoki; Yokouchi, Haruna; Mimura, Mariyo; Nakamura, Riki; Atsumi, Gen-ichi

    2015-01-01

    Aims: This study aimed to identify new hemostyptics by assessing the coagulation enhancing activity of 114 Chinese herbal extracts in vitro. Methods: Herbs were boiled in water for 30 min, filtered and then lyophilized filtrates (10 mg/mL) were dissolved in water. Coagulation was assayed as prothrombin time (PT). Plasma diluted in saline was incubated with each extract for 5 min and then PT reagent was added, followed by CaCl2 solution and the time taken to form clots was measured. Extracts that decreased coagulation time were regarded as containing active compounds. The abilities of extracts to activate Factor XII were assessed and the activated form of factor XII (XIIa) was resolved by SDS-PAGE and visualized by silver staining. Results: Coagulation time was obviously shortened by extracts of Alpinia Rhizome, Areca, Artemisia Leaf, Cassia Bark, Danshen Root, Ephedra Herb, Epimedium Herb, Forsythia Fruit, Great Burdock Achene, Moutan Bark, Perilla Herb, Red Paeony Root, Schizonepeta Spike, Senticosus Rhizome, Sweet Annie, Uncaria Thorn and Zanthoxylum Peel. Factor XII was obviously activated by extracts of Artemisia Leaf and Great Burdock Achene, and slightly by Perilla herb. Conclusion: Some popular Chinese medicinal herbs have potential as hemostatic agents and could thus be develope as new strategies for the treatment and prevention of bleeding. PMID:26401379

  18. Rapid Screening Method for Mycobactericidal Activity of Chemical Germicides That Uses Mycobacterium terrae Expressing a Green Fluorescent Protein Gene

    PubMed Central

    Zafer, Ahmed A.; Taylor, Yvonne E.; Sattar, Syed A.

    2001-01-01

    The slow growth of mycobacteria in conventional culture methods impedes the testing of chemicals for mycobactericidal activity. An assay based on expression of the green fluorescent protein (GFP) by mycobacteria was developed as a rapid alternative. Plasmid pBEN, containing the gene encoding a red-shifted, high-intensity GFP mutant, was incorporated into Mycobacterium terrae (ATCC 15755), and GFP expression was observed by epifluorescence microscopy. Mycobactericidal activity was assessed by separately exposing a suspension of M. terrae(pBEN) to several dilutions of test germicides based on 7.5% hydrogen peroxide, 2.4% alkaline glutaraldehyde, 10% acid glutaraldehyde, and 15.5% of a phenolic agent for contact times ranging from 10 to 20 min (22°C), followed by culture of the exposed cells in broth (Middlebrook 7H9) and measurement of fluorescence every 24 h. When the fluorescence was to be compared with CFU, the samples were plated on Middlebrook 7H11 agar and incubated for 4 weeks. No increase in fluorescence or CFU occurred in cultures in which the cells had been inactivated by the germicide concentrations tested. Where the test bacterium was exposed to ineffective levels of the germicides, fluorescence increased after a lag period of 1 to 7 days, corresponding to the level of bacterial inactivation. In untreated controls, fluorescence increased rapidly to reach a peak in 2 to 4 days. A good Pearson correlation coefficient (r ≥0.85) was observed between the intensity of fluorescence and the number of CFU. The GFP-based fluorescence assay reduced the turnaround time in the screening of chemical germicides for mycobactericidal activity to ≤7 days. PMID:11229916

  19. Real-Time Monitoring and Evaluation of a Visual-Based Cervical Cancer Screening Program Using a Decision Support Job Aid

    PubMed Central

    Peterson, Curtis W.; Rose, Donny; Mink, Jonah; Levitz, David

    2016-01-01

    In many developing nations, cervical cancer screening is done by visual inspection with acetic acid (VIA). Monitoring and evaluation (M&E) of such screening programs is challenging. An enhanced visual assessment (EVA) system was developed to augment VIA procedures in low-resource settings. The EVA System consists of a mobile colposcope built around a smartphone, and an online image portal for storing and annotating images. A smartphone app is used to control the mobile colposcope, and upload pictures to the image portal. In this paper, a new app feature that documents clinical decisions using an integrated job aid was deployed in a cervical cancer screening camp in Kenya. Six organizations conducting VIA used the EVA System to screen 824 patients over the course of a week, and providers recorded their diagnoses and treatments in the application. Real-time aggregated statistics were broadcast on a public website. Screening organizations were able to assess the number of patients screened, alongside treatment rates, and the patients who tested positive and required treatment in real time, which allowed them to make adjustments as needed. The real-time M&E enabled by “smart” diagnostic medical devices holds promise for broader use in screening programs in low-resource settings. PMID:27196932

  20. Real-Time Monitoring and Evaluation of a Visual-Based Cervical Cancer Screening Program Using a Decision Support Job Aid.

    PubMed

    Peterson, Curtis W; Rose, Donny; Mink, Jonah; Levitz, David

    2016-01-01

    In many developing nations, cervical cancer screening is done by visual inspection with acetic acid (VIA). Monitoring and evaluation (M&E) of such screening programs is challenging. An enhanced visual assessment (EVA) system was developed to augment VIA procedures in low-resource settings. The EVA System consists of a mobile colposcope built around a smartphone, and an online image portal for storing and annotating images. A smartphone app is used to control the mobile colposcope, and upload pictures to the image portal. In this paper, a new app feature that documents clinical decisions using an integrated job aid was deployed in a cervical cancer screening camp in Kenya. Six organizations conducting VIA used the EVA System to screen 824 patients over the course of a week, and providers recorded their diagnoses and treatments in the application. Real-time aggregated statistics were broadcast on a public website. Screening organizations were able to assess the number of patients screened, alongside treatment rates, and the patients who tested positive and required treatment in real time, which allowed them to make adjustments as needed. The real-time M&E enabled by "smart" diagnostic medical devices holds promise for broader use in screening programs in low-resource settings. PMID:27196932

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

    ERIC Educational Resources Information Center

    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…

  2. A Four-Point Screening Method for Assessing Molecular Mechanism of Action (MMOA) Identifies Tideglusib as a Time-Dependent Inhibitor of Trypanosoma brucei GSK3β

    PubMed Central

    Swinney, Zachary T.; Haubrich, Brad A.; Xia, Shuangluo; Ramesha, Chakk; Gomez, Stephen R.; Guyett, Paul; Mensa-Wilmot, Kojo; Swinney, David C.

    2016-01-01

    Background New therapeutics are needed for neglected tropical diseases including Human African trypanosomiasis (HAT), a progressive and fatal disease caused by the protozoan parasites Trypanosoma brucei gambiense and T. b. rhodesiense. There is a need for simple, efficient, cost effective methods to identify new molecules with unique molecular mechanisms of action (MMOAs). The mechanistic features of a binding mode, such as competition with endogenous substrates and time-dependence can affect the observed inhibitory IC50, and differentiate molecules and their therapeutic usefulness. Simple screening methods to determine time-dependence and competition can be used to differentiate compounds with different MMOAs in order to identify new therapeutic opportunities. Methodology/Principal Findings In this work we report a four point screening methodology to evaluate the time-dependence and competition for inhibition of GSK3β protein kinase isolated from T. brucei. Using this method, we identified tideglusib as a time-dependent inhibitor whose mechanism of action is time-dependent, ATP competitive upon initial binding, which transitions to ATP non-competitive with time. The enzyme activity was not recovered following 100-fold dilution of the buffer consistent with an irreversible mechanism of action. This is in contrast to the T. brucei GSK3β inhibitor GW8510, whose inhibition was competitive with ATP, not time-dependent at all measured time points and reversible in dilution experiments. The activity of tideglusib against T. brucei parasites was confirmed by inhibition of parasite proliferation (GI50 of 2.3 μM). Conclusions/Significance Altogether this work demonstrates a straightforward method for determining molecular mechanisms of action and its application for mechanistic differentiation of two potent TbGSK3β inhibitors. The four point MMOA method identified tideglusib as a mechanistically differentiated TbGSK3β inhibitor. Tideglusib was shown to inhibit parasite

  3. Non-target time trend screening: a data reduction strategy for detecting emerging contaminants in biological samples.

    PubMed

    Plassmann, Merle M; Tengstrand, Erik; Åberg, K Magnus; Benskin, Jonathan P

    2016-06-01

    Non-targeted mass spectrometry-based approaches for detecting novel xenobiotics in biological samples are hampered by the occurrence of naturally fluctuating endogenous substances, which are difficult to distinguish from environmental contaminants. Here, we investigate a data reduction strategy for datasets derived from a biological time series. The objective is to flag reoccurring peaks in the time series based on increasing peak intensities, thereby reducing peak lists to only those which may be associated with emerging bioaccumulative contaminants. As a result, compounds with increasing concentrations are flagged while compounds displaying random, decreasing, or steady-state time trends are removed. As an initial proof of concept, we created artificial time trends by fortifying human whole blood samples with isotopically labelled standards. Different scenarios were investigated: eight model compounds had a continuously increasing trend in the last two to nine time points, and four model compounds had a trend that reached steady state after an initial increase. Each time series was investigated at three fortification levels and one unfortified series. Following extraction, analysis by ultra performance liquid chromatography high-resolution mass spectrometry, and data processing, a total of 21,700 aligned peaks were obtained. Peaks displaying an increasing trend were filtered from randomly fluctuating peaks using time trend ratios and Spearman's rank correlation coefficients. The first approach was successful in flagging model compounds spiked at only two to three time points, while the latter approach resulted in all model compounds ranking in the top 11 % of the peak lists. Compared to initial peak lists, a combination of both approaches reduced the size of datasets by 80-85 %. Overall, non-target time trend screening represents a promising data reduction strategy for identifying emerging bioaccumulative contaminants in biological samples. Graphical abstract

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

    PubMed

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

    2015-09-01

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

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

    PubMed Central

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

    2015-01-01

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

  6. Specific Antivirulence Activity, A New Concept for Reliable Screening of Virulence Inhibitors.

    PubMed

    Defoirdt, Tom

    2016-07-01

    Antivirulence therapy, disarming pathogens rather than killing them, is emerging as a novel strategy for disease control. Reporter strains expressing an easily measurable and quantifiable phenotype enable easy screening of virulence inhibitors. In this paper I propose a novel concept to exclude false positives in this type of screening. PMID:26879186

  7. Time Perspective and Physical Activity among Central Appalachian Adolescents

    ERIC Educational Resources Information Center

    Gulley, Tauna

    2013-01-01

    Time perspective is a cultural behavioral concept that reflects individuals' orientations or attitudes toward the past, present, or future. Individuals' time perspectives influence their choices regarding daily activities. Time perspective is an important consideration when teaching adolescents about the importance of being physically…

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

    PubMed

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

    2016-02-01

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

  9. Informed Choice in the German Mammography Screening Program by Education and Migrant Status: Survey among First-Time Invitees

    PubMed Central

    Berens, Eva-Maria; Reder, Maren; Razum, Oliver; Kolip, Petra; Spallek, Jacob

    2015-01-01

    Breast cancer is the most prevalent cancer among women and mammography screening programs are seen as a key strategy to reduce breast cancer mortality. In Germany, women are invited to the population-based mammography screening program between ages 50 to 69. It is still discussed whether the benefits of mammography screening outweigh its harms. Therefore, the concept of informed choice comprising knowledge, attitude and intention has gained importance. The objective of this observational study was to assess the proportion of informed choices among women invited to the German mammography screening program for the first time. A representative sample of 17,349 women aged 50 years from a sub-region of North Rhine Westphalia was invited to participate in a postal survey. Turkish immigrant women were oversampled. The effects of education level and migration status on informed choice and its components were assessed. 5,847 (33.7%) women responded to the postal questionnaire of which 4,113 were used for analyses. 31.5% of the women had sufficient knowledge. The proportion of sufficient knowledge was lower among immigrants and among women with low education levels. The proportion of women making informed choices was low (27.1%), with similar associations with education level and migration status. Women of low (OR 2.75; 95% CI 2.18–3.46) and medium education level (OR 1.49; 95% CI 1.27–1.75) were more likely to make an uninformed choice than women of high education level. Turkish immigrant women had the greatest odds for making an uninformed choice (OR 5.30, 95% CI 1.92–14.66) compared to non-immigrant women. Other immigrant women only had slightly greater odds for making an uninformed choice than non-immigrant women. As immigrant populations and women with low education level have been shown to have poor knowledge, they need special attention in measures to increase knowledge and thus informed choices. PMID:26529513

  10. What's on Your Radar Screen? Distance-Rate-Time Problems from NASA

    ERIC Educational Resources Information Center

    Condon, Gregory W.; Landesman, Miriam F.; Calasanz-Kaiser, Agnes

    2006-01-01

    This article features NASA's FlyBy Math, a series of six standards-based distance-rate-time investigations in air traffic control. Sixth-grade students--acting as pilots, air traffic controllers, and NASA scientists--conduct an experiment and then use multiple mathematical representations to analyze and solve a problem involving two planes flying…

  11. American Time Use Survey: Sleep Time and Its Relationship to Waking Activities

    PubMed Central

    Basner, Mathias; Fomberstein, Kenneth M.; Razavi, Farid M.; Banks, Siobhan; William, Jeffrey H.; Rosa, Roger R.; Dinges, David F.

    2007-01-01

    Study Objectives: To gain some insight into how various behavioral (lifestyle) factors influence sleep duration, by investigation of the relationship of sleep time to waking activities using the American Time Use Survey (ATUS). Design: Cross-sectional data from ATUS, an annual telephone survey of a population sample of US citizens who are interviewed regarding how they spent their time during a 24-hour period between 04:00 on the previous day and 04:00 on the interview day. Participants: Data were pooled from the 2003, 2004, and 2005 ATUS databases involving N=47,731 respondents older than 14 years of age. Interventions: N/A Results: Adjusted multiple linear regression models showed that the largest reciprocal relationship to sleep was found for work time, followed by travel time, which included commute time. Only shorter than average sleepers (<7.5 h) spent more time socializing, relaxing, and engaging in leisure activities, while both short (<5.5 h) and long sleepers (≥8.5 h) watched more TV than the average sleeper. The extent to which sleep time was exchanged for waking activities was also shown to depend on age and gender. Sleep time was minimal while work time was maximal in the age group 45–54 yr, and sleep time increased both with lower and higher age. Conclusions: Work time, travel time, and time for socializing, relaxing, and leisure are the primary activities reciprocally related to sleep time among Americans. These activities may be confounding the frequently observed association between short and long sleep on one hand and morbidity and mortality on the other hand and should be controlled for in future studies. Citation: Basner M; Fomberstein KM; Razavi FM; Banks S; William JH; Rosa RR; Dinges DF. American time use survey: sleep time and its relationship to waking activities. SLEEP 2007;30(9):1085-1095. PMID:17910380

  12. Genetic screening

    PubMed Central

    Andermann, Anne; Blancquaert, Ingeborg

    2010-01-01

    Abstract OBJECTIVE To provide a primer for primary care professionals who are increasingly called upon to discuss the growing number of genetic screening services available and to help patients make informed decisions about whether to participate in genetic screening, how to interpret results, and which interventions are most appropriate. QUALITY OF EVIDENCE As part of a larger research program, a wide literature relating to genetic screening was reviewed. PubMed and Internet searches were conducted using broad search terms. Effort was also made to identify the gray literature. MAIN MESSAGE Genetic screening is a type of public health program that is systematically offered to a specified population of asymptomatic individuals with the aim of providing those identified as high risk with prevention, early treatment, or reproductive options. Ensuring an added benefit from screening, as compared with standard clinical care, and preventing unintended harms, such as undue anxiety or stigmatization, depends on the design and implementation of screening programs, including the recruitment methods, education and counseling provided, timing of screening, predictive value of tests, interventions available, and presence of oversight mechanisms and safeguards. There is therefore growing apprehension that economic interests might lead to a market-driven approach to introducing and expanding screening before program effectiveness, acceptability, and feasibility have been demonstrated. As with any medical intervention, there is a moral imperative for genetic screening to do more good than harm, not only from the perspective of individuals and families, but also for the target population and society as a whole. CONCLUSION Primary care professionals have an important role to play in helping their patients navigate the rapidly changing terrain of genetic screening services by informing them about the benefits and risks of new genetic and genomic technologies and empowering them to

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

    PubMed

    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. PMID:26340935

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

    PubMed Central

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

    2013-01-01

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

  15. The Role of Activated Nitrogen Species on Double-folded Screen Nitriding Process

    NASA Astrophysics Data System (ADS)

    Kim, Sanggweon; Lee, Jaehoon; Saito, Nagahiro; Takai, Osamu

    2013-03-01

    As clean and energy saving surface hardening technology, plasma nitriding techniques have been evolved with object of higher performance in the last decades. Even though the diffusion of nitrogen inward to steel is occurred at the final step, solid diffusion from surface, energy transition from gas molecule of nitrogen to atomic or an activated state have many different steps depending on the plasma conditions, parameters and the design of each equipment. And this study made comparative on nitrogen sources transfer with conventional DC plasma nitriding and novel nitriding process using plasma diagnosis and metallurgical observation. With different vacuum pressure, gas ratio and new designed electrode (double-folded screen cathode electrode), it showed a different behavior of DC plasma nitriding including the nano-sized nitride on the outer surface of specimen due to nitrogen source of determining plasma species. In this study, plasma species was able to identify with optical emission spectroscopy (OES) studies. From these observations, we could understand better role of ions or neutral nitrogen species, like neutral nitrogen (N), N2+ and NHx radicals in plasma nitriding process with different parameters. And cutting layers of nitride specimen were showed the results due to a different species gas flow ratio or plasma conditions.

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

    PubMed Central

    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

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

    PubMed

    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

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

    PubMed

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

    2006-01-16

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

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

    PubMed

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

    2015-07-01

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

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

    PubMed

    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. PMID:26791508

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

    PubMed

    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. PMID:27116029

  2. Development of a comprehensive spectral library of sildenafil and related active analogues using LC-QTOF-MS and its application for screening counterfeit pharmaceuticals.

    PubMed

    Lee, Sooyeun; Ji, Dajeong; Park, Meejung; Chung, Kyu Hyuck

    2015-12-01

    The abuse or misuse of forged erectile-dysfunction drugs, containing phosphodiesterase type 5 inhibitors (e.g. sildenafil), is a serious issue globally. Therefore, the detection of sildenafil and related active analogues in counterfeit pharmaceuticals or the differentiation between counterfeit and authentic drugs has been performed with a variety of analytical techniques. Recently, a liquid chromatography-hybrid quadrupole time-of-flight mass spectrometry (LC-QTOF-MS)-based in-house library, consisting of accurate mass ion fragmentation information and retention times, was effectively applied to screen a large number of compounds in field of forensic toxicology. However, a comprehensive LC-QTOF-MS spectral library of sildenafil and related active analogues has not yet been reported. In the present study, a spectral library of 40 compounds of sildenafil and related analogues was developed with accurate mass spectra and retention times using LC-QTOF-MS, and applied to screen nine marketed counterfeit products. The in-house library successfully identified sildenafil, dimethylsildenafil, hydroxyhomosildenafil, demethylhongdenafil, pseudovardenafil and vardenafil in the samples. Our LC-QTOF-MS-based spectral library search is considered a powerful approach for identifying sildenafil and related active analogues in counterfeit pharmaceuticals. PMID:26363440

  3. Design and screening of a chimeric survivin-specific nanobody and its anticancer activities in vitro.

    PubMed

    Zhang, Na; Guo, Hua; Zheng, Wenyun; Wang, Tianwen; Ma, Xingyuan

    2016-10-01

    Survivin is a strong inhibitor of apoptosis protein and a promising target for cancer prevention and treatment. Here, we report the design and preparation of novel chimeric nanobodies (Nbs) that could specifically bind to survivin. We screened the peptides from phage-displayed libraries (7-mer, 12-mer) for nonconserved sequences of complementarity-determining regions (CDRs) in the scaffold of the Nb. By a combination of the nonconserved sequences for CDRs, the corresponding chimeric Nbs (10 Nbs) were prepared with genetic operations. The antisurvivin Nb TAT-Nb4A (a fusion with cellular transduction peptide TAT) was found to be the most efficient antibody on the basis of the results from enzyme-linked immunosorbent assay, MTT, and flow cytometry when these nanobodies were tested with hepatoma carcinoma cell HepG2. TAT-Nb4A could inhibit the growth of HepG2 and promote cancer cell apoptosis significantly in a dose-dependent and time-dependent manner: the apoptosis rate reached 52.5% when the concentration of TAT-Nb4A was 120 μg/ml. Western blotting with cells expressing survivin showed that the prepared nanobody could efficiently bind to expressed survivin and blocked the signaling pathway in which survivin played a role. This study provided a convenient and feasible method of obtaining a novel specific Nb with the case of survivin as a good example. PMID:27362789

  4. Fluorescence-based screening of cytochrome P450 activities in intact cells.

    PubMed

    Donato, M Teresa; Gómez-Lechón, M José

    2013-01-01

    Fluorimetric methods to assess cytochrome P450 (P450) activities that do not require metabolite separation have been developed. These methods make use of non- or low-fluorescent P450 substrates that produce highly fluorescent metabolites in aqueous solutions. The assays are based on the direct incubation of intact cells in culture with appropriate fluorogenic probe substrates, followed by fluorimetric quantification of the product formed and released into incubation medium. We describe a battery of fluorescence assays for rapid measurement of the activity of nine P450s involved in drug metabolism. For each individual P450 activity the probe showing the best properties (highest metabolic rates, lowest background fluorescence) has been selected. Fluorescence-based assays are highly sensitive and allow the simultaneous activity assessments of cells cultured in 96-well plates, using plate readers, with notable reductions in costs, time, and cells, thus enhancing sample throughput. PMID:23475674

  5. A novel, sensitive assay for high-throughput molecular detection of plasmodia for active screening of malaria for elimination.

    PubMed

    Cheng, Zhibin; Sun, Xiaodong; Yang, Ye; Wang, Heng; Zheng, Zhi

    2013-01-01

    Although malaria remains one of the leading infectious diseases in the world, the decline in malaria transmission in some area makes it possible to consider elimination of the disease. As countries approach elimination, malaria diagnosis needs to change from diagnosing ill patients to actively detecting infections in all carriers, including asymptomatic and low-parasite-load patients. However, few of the current diagnostic methods have both the throughput and the sensitivity required. We adopted a sandwich RNA hybridization assay to detect genus Plasmodium 18S rRNA directly from whole-blood samples from Plasmodium falciparum and Plasmodium vivax patients without RNA isolation. We tested the assay with 202 febrile patients from areas where malaria is endemic, using 20 μl of each blood sample in a 96-well plate format with a 2-day enzyme-linked immunosorbent assay (ELISA)-like work flow. The results were compared with diagnoses obtained using microscopy, a rapid diagnostic test (RDT), and genus-specific real-time PCR. Our assay identified all 66 positive samples diagnosed by microscopy, including 49 poorly stored samples that underwent multiple freeze-thaw cycles due to resource limitation. The assay uncovered three false-negative samples by microscopy and four false-negative samples by RDT and agreed completely with real-time PCR diagnosis. There was no negative sample by our assay that would show a positive result when tested with other methods. The detection limit of our assay for P. falciparum was 0.04 parasite/μl. The assay's simple work flow, high throughput, and sensitivity make it suitable for active malaria screening. PMID:23100347

  6. The Elasticity of Time: Associations between Physical Activity and Use of Time in Adolescents

    ERIC Educational Resources Information Center

    Olds, Tim; Ferrar, Katia E.; Gomersall, Sjaan R.; Maher, Carol; Walters, J. L.

    2012-01-01

    The way an individual uses one's time can greatly affect his or her health. The purpose of this article was to examine the cross-sectional cross-elasticity relationships for use of time domains in a sample of Australian adolescents. This study analyzed 24-hour recall time use data collected using the Multimedia Activity Recall for Children and…

  7. Development of a qualitative, multiplex real-time PCR kit for screening of genetically modified organisms (GMOs).

    PubMed

    Dörries, Hans-Henno; Remus, Ivonne; Grönewald, Astrid; Grönewald, Cordt; Berghof-Jäger, Kornelia

    2010-03-01

    The number of commercially available genetically modified organisms (GMOs) and therefore the diversity of possible target sequences for molecular detection techniques are constantly increasing. As a result, GMO laboratories and the food production industry currently are forced to apply many different methods to reliably test raw material and complex processed food products. Screening methods have become more and more relevant to minimize the analytical effort and to make a preselection for further analysis (e.g., specific identification or quantification of the GMO). A multiplex real-time PCR kit was developed to detect the 35S promoter of the cauliflower mosaic virus, the terminator of the nopaline synthase gene of Agrobacterium tumefaciens, the 35S promoter from the figwort mosaic virus, and the bar gene of the soil bacterium Streptomyces hygroscopicus as the most widely used sequences in GMOs. The kit contains a second assay for the detection of plant-derived DNA to control the quality of the often processed and refined sample material. Additionally, the plant-specific assay comprises a homologous internal amplification control for inhibition control. The determined limits of detection for the five assays were 10 target copies/reaction. No amplification products were observed with DNAs of 26 bacterial species, 25 yeasts, 13 molds, and 41 not genetically modified plants. The specificity of the assays was further demonstrated to be 100% by the specific amplification of DNA derived from reference material from 22 genetically modified crops. The applicability of the kit in routine laboratory use was verified by testing of 50 spiked and unspiked food products. The herein described kit represents a simple and sensitive GMO screening method for the reliable detection of multiple GMO-specific target sequences in a multiplex real-time PCR reaction. PMID:19798485

  8. Identification of benzopyrone as a common structural feature in compounds with anti-inflammatory activity in a zebrafish phenotypic screen

    PubMed Central

    Robertson, Anne L.; Ogryzko, Nikolay V.; Henry, Katherine M.; Loynes, Catherine A.; Foulkes, Matthew J.; Meloni, Marco M.; Wang, Xingang; Ford, Christopher; Jackson, Malcolm; Ingham, Philip W.; Wilson, Heather L.; Farrow, Stuart N.; Solari, Roberto; Flower, Roderick J.; Jones, Simon; Whyte, Moira K. B.

    2016-01-01

    ABSTRACT Neutrophils are essential for host defence and are recruited to sites of inflammation in response to tissue injury or infection. For inflammation to resolve, these cells must be cleared efficiently and in a controlled manner, either by apoptosis or reverse migration. If the inflammatory response is not well-regulated, persistent neutrophils can cause damage to host tissues and contribute to the pathogenesis of chronic inflammatory diseases, which respond poorly to current treatments. It is therefore important to develop drug discovery strategies that can identify new therapeutics specifically targeting neutrophils, either by promoting their clearance or by preventing their recruitment. Our recent in vivo chemical genetic screen for accelerators of inflammation resolution identified a subset of compounds sharing a common chemical signature, the bicyclic benzopyrone rings. Here, we further investigate the mechanisms of action of the most active of this chemical series, isopimpinellin, in our zebrafish model of neutrophilic inflammation. We found that this compound targets both the recruitment and resolution phases of the inflammatory response. Neutrophil migration towards a site of injury is reduced by isopimpinellin and this occurs as a result of PI3K inhibition. We also show that isopimpinellin induces neutrophil apoptosis to drive inflammation resolution in vivo using a new zebrafish reporter line detecting in vivo neutrophil caspase-3 activity and allowing quantification of flux through the apoptotic pathway in real time. Finally, our studies reveal that clinically available ‘cromones’ are structurally related to isopimpinellin and have previously undescribed pro-resolution activity in vivo. These findings could have implications for the therapeutic use of benzopyrones in inflammatory disease. PMID:27079522

  9. Identification of benzopyrone as a common structural feature in compounds with anti-inflammatory activity in a zebrafish phenotypic screen.

    PubMed

    Robertson, Anne L; Ogryzko, Nikolay V; Henry, Katherine M; Loynes, Catherine A; Foulkes, Matthew J; Meloni, Marco M; Wang, Xingang; Ford, Christopher; Jackson, Malcolm; Ingham, Philip W; Wilson, Heather L; Farrow, Stuart N; Solari, Roberto; Flower, Roderick J; Jones, Simon; Whyte, Moira K B; Renshaw, Stephen A

    2016-06-01

    Neutrophils are essential for host defence and are recruited to sites of inflammation in response to tissue injury or infection. For inflammation to resolve, these cells must be cleared efficiently and in a controlled manner, either by apoptosis or reverse migration. If the inflammatory response is not well-regulated, persistent neutrophils can cause damage to host tissues and contribute to the pathogenesis of chronic inflammatory diseases, which respond poorly to current treatments. It is therefore important to develop drug discovery strategies that can identify new therapeutics specifically targeting neutrophils, either by promoting their clearance or by preventing their recruitment. Our recent in vivo chemical genetic screen for accelerators of inflammation resolution identified a subset of compounds sharing a common chemical signature, the bicyclic benzopyrone rings. Here, we further investigate the mechanisms of action of the most active of this chemical series, isopimpinellin, in our zebrafish model of neutrophilic inflammation. We found that this compound targets both the recruitment and resolution phases of the inflammatory response. Neutrophil migration towards a site of injury is reduced by isopimpinellin and this occurs as a result of PI3K inhibition. We also show that isopimpinellin induces neutrophil apoptosis to drive inflammation resolution in vivo using a new zebrafish reporter line detecting in vivo neutrophil caspase-3 activity and allowing quantification of flux through the apoptotic pathway in real time. Finally, our studies reveal that clinically available 'cromones' are structurally related to isopimpinellin and have previously undescribed pro-resolution activity in vivo These findings could have implications for the therapeutic use of benzopyrones in inflammatory disease. PMID:27079522

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

    PubMed Central

    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

  11. Effector kinase coupling enables high-throughput screens for direct HIV-1 Nef antagonists with antiretroviral activity.

    PubMed

    Emert-Sedlak, Lori A; Narute, Purushottam; Shu, Sherry T; Poe, Jerrod A; Shi, Haibin; Yanamala, Naveena; Alvarado, John Jeff; Lazo, John S; Yeh, Joanne I; Johnston, Paul A; Smithgall, Thomas E

    2013-01-24

    HIV-1 Nef, a critical AIDS progression factor, represents an important target protein for antiretroviral drug discovery. Because Nef lacks intrinsic enzymatic activity, we developed an assay that couples Nef to the activation of Hck, a Src family member and Nef effector protein. Using this assay, we screened a large, diverse chemical library and identified small molecules that block Nef-dependent Hck activity with low micromolar potency. Of these, a diphenylpyrazolo compound demonstrated submicromolar potency in HIV-1 replication assays against a broad range of primary Nef variants. This compound binds directly to Nef via a pocket formed by the Nef dimerization interface and disrupts Nef dimerization in cells. Coupling of nonenzymatic viral accessory factors to host cell effector proteins amenable to high-throughput screening may represent a general strategy for the discovery of new antimicrobial agents. PMID:23352142

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

    PubMed Central

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

    2007-01-01

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

  13. Screen-based media use clusters are related to other activity behaviours and health indicators in adolescents

    PubMed Central

    2013-01-01

    Background Screen-based media (SBM) occupy a considerable portion of young peoples’ discretionary leisure time. The aim of this paper was to investigate whether distinct clusters of SBM use exist, and if so, to examine the relationship of any identified clusters with other activity/sedentary behaviours and physical and mental health indicators. Methods The data for this study come from 643 adolescents, aged 14 years, who were participating in the longitudinal Western Australian Pregnancy Cohort (Raine) Study through May 2003 to June 2006. Time spent on SBM, phone use and reading was assessed using the Multimedia Activity Recall for Children and Adults. Height, weight, muscle strength were measured at a clinic visit and the adolescents also completed questionnaires on their physical activity and psychosocial health. Latent class analysis (LCA) was used to analyse groupings of SBM use. Results Three clusters of SBM use were found; C1 ‘instrumental computer users’ (high email use, general computer use), C2 ‘multi-modal e-gamers’ (both high console and computer game use) and C3 ‘computer e-gamers’ (high computer game use only). Television viewing was moderately high amongst all the clusters. C2 males took fewer steps than their male peers in C1 and C3 (-13,787/week, 95% CI: -4619 to -22957, p = 0.003 and -14,806, 95% CI: -5,306 to -24,305, p = 0.002) and recorded less MVPA than the C1 males (-3.5 h, 95% CI: -1.0 to -5.9, p = 0.005). There was no difference in activity levels between females in clusters C1 and C3. Conclusion SBM use by adolescents did cluster and these clusters related differently to activity/sedentary behaviours and both physical and psychosocial health indicators. It is clear that SBM use is not a single construct and future research needs to take consideration of this if it intends to understand the impact SBM has on health. PMID:24330626

  14. Multi-Channel Microfluidic Biosensor Platform Applied for Online Monitoring and Screening of Biofilm Formation and Activity

    PubMed Central

    Bruchmann, Julia; Sachsenheimer, Kai; Rapp, Bastian E.; Schwartz, Thomas

    2015-01-01

    Bacterial colonization of surfaces and interfaces has a major impact on various areas including biotechnology, medicine, food industries, and water technologies. In most of these areas biofilm development has a strong impact on hygiene situations, product quality, and process efficacies. In consequence, biofilm manipulation and prevention is a fundamental issue to avoid adverse impacts. For such scenario online, non-destructive biofilm monitoring systems become important in many technical and industrial applications. This study reports such a system in form of a microfluidic sensor platform based on the combination of electrical impedance spectroscopy and amperometric current measurement, which allows sensitive online measurement of biofilm formation and activity. A total number of 12 parallel fluidic channels enable real-time online screening of various biofilms formed by different Pseudomonas aeruginosa and Stenotrophomonas maltophilia strains and complex mixed population biofilms. Experiments using disinfectant and antibiofilm reagents demonstrate that the biofilm sensor is able to discriminate between inactivation/killing of bacteria and destabilization of biofilm structures. The impedance and amperometric sensor data demonstrated the high dynamics of biofilms as a consequence of distinct responses to chemical treatment strategies. Gene expression of flagellar and fimbrial genes of biofilms grown inside the microfluidic system supported the detected biofilm growth kinetics. Thus, the presented biosensor platform is a qualified tool for assessing biofilm formation in specific environments and for evaluating the effectiveness of antibiofilm treatment strategies. PMID:25706987

  15. High-Throughput Screening for Internalizing Antibodies by Homogeneous Fluorescence Imaging of a pH-Activated Probe

    PubMed Central

    Riedl, Thilo; van Boxtel, Egon; Bosch, Martijn; Parren, Paul W. H. I.; Gerritsen, Arnout F.

    2016-01-01

    Antibody-drug conjugates (ADCs) represent a rapidly growing class of biotherapeutics that deliver drugs specifically to target cells by binding of the antibody component to surface receptors. The majority of ADCs require receptor internalization depending on intrinsic features of the specific ADC-antigen interaction. The development of potent ADCs would greatly benefit from the identification of efficiently internalizing antibodies at early stages of discovery. We developed a highly sensitive and rapid antibody internalization assay using an indirect Cypher5E label. The pH-activated CypHer5E label becomes fluorescent upon internalization into the acidic environment of endocytic organelles, whereas background fluorescence of noninternalized CypHer5E is minimal. The pH-dependency of the CypHer5E signal enables robust discrimination of antibody internalization from surface binding. The favorable signal-over-background ratio allows a homogeneous assay design with high-throughput fluorescence imaging in 384- and 1536-well formats. The biophysical readout of the primary internalization event substantially shortens incubation times compared to killing assays using toxin internalization. The assay was validated with tumor-relevant targets, including receptor tyrosine kinases (EGFR and HER2) and a class II cytokine receptor (TF) expressed by A431, AU565, and SKOV-3 cells and transient expression systems (CHO-S). Our method enables functional screening of large antibody libraries to identify therapeutic antibody candidates with internalization characteristics favorable for the development of ADCs. PMID:26518032

  16. Multi-channel microfluidic biosensor platform applied for online monitoring and screening of biofilm formation and activity.

    PubMed

    Bruchmann, Julia; Sachsenheimer, Kai; Rapp, Bastian E; Schwartz, Thomas

    2015-01-01

    Bacterial colonization of surfaces and interfaces has a major impact on various areas including biotechnology, medicine, food industries, and water technologies. In most of these areas biofilm development has a strong impact on hygiene situations, product quality, and process efficacies. In consequence, biofilm manipulation and prevention is a fundamental issue to avoid adverse impacts. For such scenario online, non-destructive biofilm monitoring systems become important in many technical and industrial applications. This study reports such a system in form of a microfluidic sensor platform based on the combination of electrical impedance spectroscopy and amperometric current measurement, which allows sensitive online measurement of biofilm formation and activity. A total number of 12 parallel fluidic channels enable real-time online screening of various biofilms formed by different Pseudomonas aeruginosa and Stenotrophomonas maltophilia strains and complex mixed population biofilms. Experiments using disinfectant and antibiofilm reagents demonstrate that the biofilm sensor is able to discriminate between inactivation/killing of bacteria and destabilization of biofilm structures. The impedance and amperometric sensor data demonstrated the high dynamics of biofilms as a consequence of distinct responses to chemical treatment strategies. Gene expression of flagellar and fimbrial genes of biofilms grown inside the microfluidic system supported the detected biofilm growth kinetics. Thus, the presented biosensor platform is a qualified tool for assessing biofilm formation in specific environments and for evaluating the effectiveness of antibiofilm treatment strategies. PMID:25706987

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

    NASA Astrophysics Data System (ADS)

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

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

  18. Quantitative high-throughput screening: A titration-based approach that efficiently identifies biological activities in large chemical libraries

    PubMed Central

    Inglese, James; Auld, Douglas S.; Jadhav, Ajit; Johnson, Ronald L.; Simeonov, Anton; Yasgar, Adam; Zheng, Wei; Austin, Christopher P.

    2006-01-01

    High-throughput screening (HTS) of chemical compounds to identify modulators of molecular targets is a mainstay of pharmaceutical development. Increasingly, HTS is being used to identify chemical probes of gene, pathway, and cell functions, with the ultimate goal of comprehensively delineating relationships between chemical structures and biological activities. Achieving this goal will require methodologies that efficiently generate pharmacological data from the primary screen and reliably profile the range of biological activities associated with large chemical libraries. Traditional HTS, which tests compounds at a single concentration, is not suited to this task, because HTS is burdened by frequent false positives and false negatives and requires extensive follow-up testing. We have developed a paradigm, quantitative HTS (qHTS), tested with the enzyme pyruvate kinase, to generate concentration–response curves for >60,000 compounds in a single experiment. We show that this method is precise, refractory to variations in sample preparation, and identifies compounds with a wide range of activities. Concentration–response curves were classified to rapidly identify pyruvate kinase activators and inhibitors with a variety of potencies and efficacies and elucidate structure–activity relationships directly from the primary screen. Comparison of qHTS with traditional single-concentration HTS revealed a high prevalence of false negatives in the single-point screen. This study demonstrates the feasibility of qHTS for accurately profiling every compound in large chemical libraries (>105 compounds). qHTS produces rich data sets that can be immediately mined for reliable biological activities, thereby providing a platform for chemical genomics and accelerating the identification of leads for drug discovery. PMID:16864780

  19. Circadian Activity Rhythms, Time Urgency, and Achievement Concerns.

    ERIC Educational Resources Information Center

    Watts, Barbara L.

    Many physiological and psychological processes fluctuate throughout the day in fairly stable, rhythmic patterns. The relationship between individual differences in circadian activity rhythms and a sense of time urgency were explored as well as a number of achievement-related variables. Undergraduates (N=308), whose circadian activity rhythms were…

  20. A Wearable Microwave Antenna Array for Time-Domain Breast Tumor Screening.

    PubMed

    Porter, Emily; Bahrami, Hadi; Santorelli, Adam; Gosselin, Benoit; Rusch, Leslie A; Popovic, Milica

    2016-06-01

    In this work, we present a clinical prototype with a wearable patient interface for microwave breast cancer detection. The long-term aim of the prototype is a breast health monitoring application. The system operates using multistatic time-domain pulsed radar, with 16 flexible antennas embedded into a bra. Unlike the previously reported, table-based prototype with a rigid cup-like holder, the wearable one requires no immersion medium and enables simple localization of breast surface. In comparison with the table-based prototype, the wearable one is also significantly more cost-effective and has a smaller footprint. To demonstrate the improved functionality of the wearable prototype, we here report the outcome of daily testing of the new, wearable prototype on a healthy volunteer over a 28-day period. The resulting data (both signals and reconstructed images) is compared to that obtained with our table-based prototype. We show that the use of the wearable prototype has improved the quality of collected volunteer data by every investigated measure. This work demonstrates the proof-of-concept for a wearable breast health monitoring array, which can be further optimized in the future for use with patients with various breast sizes and tissue densities. PMID:26780788

  1. Predicting antitrichomonal activity: a computational screening using atom-based bilinear indices and experimental proofs.

    PubMed

    Marrero-Ponce, Yovani; Meneses-Marcel, Alfredo; Castillo-Garit, Juan A; Machado-Tugores, Yanetsy; Escario, José Antonio; Barrio, Alicia Gómez; Pereira, David Montero; Nogal-Ruiz, Juan José; Arán, Vicente J; Martínez-Fernández, Antonio R; Torrens, Francisco; Rotondo, Richard; Ibarra-Velarde, Froylán; Alvarado, Ysaias J

    2006-10-01

    classification functions were then applied to find new lead antitrichomonal agents and six compounds were selected as possible active compounds by computational screening. The designed compounds were synthesized and tested for in vitro activity against T. vaginalis. Out of the six compounds that were designed, and synthesized, three molecules (chemicals VA5-5a, VA5-5c, and VA5-12b) showed high to moderate cytocidal activity at the concentration of 10 microg/ml, other two compounds (VA5-8pre and VA5-8) showed high cytocidal and cytostatic activity at the concentration of 100 microg/ml and 10 microg/ml, correspondingly, and the remaining chemical (compound VA5-5e) was inactive at these assayed concentrations. Nonetheless, these compounds possess structural features not seen in known trichomonacidal compounds and thus can serve as excellent leads for further optimization of antitrichomonal activity. The LDA-based QSAR models presented here can be considered as a computer-assisted system that could potentially significantly reduce the number of synthesized and tested compounds and increase the chance of finding new chemical entities with antitrichomonal activity. PMID:16875830

  2. Evaluation of a carp primary hepatocyte culture system for screening chemicals for oestrogenic activity.

    PubMed

    Bickley, L K; Lange, A; Winter, M J; Tyler, C R

    2009-09-14

    The presence of endocrine disrupting chemicals (EDCs) in the environment has driven the development of screening and testing assays to both identify chemicals with hormonal activity and evaluate their potential to cause adverse effects. As the number of animals used for research and regulatory purposes rises, and set against a desire to reduce animal testing, there is increased emphasis on the development and application of in vitro techniques to evaluate chemical risks to the environment. Induction of vitellogenin (VTG) in isolated fish liver cells has been used successfully to identify a wide range of EDCs, including both natural and synthetic oestrogens and a variety of other xenoestrogens. However, the vitellogenic response reported for hepatocytes in culture has been shown to vary widely, making comparisons between studies difficult. The work presented in this paper explored the variability of the vitellogenic response in primary cultures of common carp (Cyprinus carpio) hepatocytes following exposure to the model oestrogenic compound, 17beta-oestradiol (E2). As expected, variability in the vitellogenic response was observed, both in terms of the sensitivity and magnitude of VTG induction, for hepatocytes isolated from different fish. An apparent difference was observed in the response of isolated hepatocytes based on the sex of the donor fish; maximum levels of E2-stimulated VTG synthesis in hepatocytes derived from females appeared higher (1962 ng mL(-1)+/-487 [n=9] compared with 1194 ng mL(-1)+/-223 for hepatocytes from males [n=9]) and EC(50) values lower (1.61+/-0.4 microM E2 for females and 2.12+/-0.2 microM E2 for males). However, these differences were not statistically significant, likely in part due to the variation observed in the vitellogenic response. In particular, hepatocytes derived from female fish showed more variation than their male counterparts (the co-efficient of variation for females was 77% compared to 28% for males). Despite the

  3. Phytochemical screening and evaluation of antioxidant activities of Dracocephalum kotschyi and determination of its luteolin content

    PubMed Central

    Kamali, Mansureh; Khosroyar, Susan; Kamali, Hossein; Ahmadzadeh Sani, Tooba; Mohammadi, Ameneh

    2016-01-01

    Objective: Dracocephalum kotschyi (Lamiaceae family) has been used in traditional medicine for stomach and liver disorders, headache and congestion. In the present study, we have investigated phytochemical properties and antioxidant activities of dichloromethane, ethyl acetate and methanol extracts of D.kotschyi. Material and Methods: Antioxidant activities of extracts were evaluated using the integration of HPLC-DPPH and ferric reducing antioxidant power (FRAP) methods. In addition, the luteolincontent was determined using HPLC method. Results: The highest antioxidant activity was observed for the methanol extract (among the three tested extracts) showing 50% DPPH scavenging activity at 4.85µg/ml as compared to butylated hydroxy toluene (BHT) and ascorbic acid (3.00 µg/ml, 0.97 µg/ml). Also, luteolin was detected in methanol extract; it was identified by comparing its retention time and DAD spectra with standard and it was one of antioxidant components of this plant. In addition, the antioxidant activity of methanol extract was higher than BHT, in FRAP assay. Total phenolic content was in the range of 11.62-22.29 mg Gallic acid /gram of dry extract and flavonoid content was in the range of 3.97-5.042 mg Quercetin/ gram of extract for dichloromethane, ethyl acetate and methanol extracts. The quantity of luteolin in D.kotschyiwas found to be 1061.005 µg/g of dried plant. Conclusion: The results of this investigation indicated that luteolin plays major role in the antioxidant activity of the plant. PMID:27516983

  4. Use of dyes in solid medium for screening ligninolytic activity of selective actinomycetes

    SciTech Connect

    Chahal, D.S.; Kluepfel, D.; Morosoli, R.

    1995-12-31

    Lignin, a three-dimensional biopolymer, not only encrusts the cellulose microfibrils in a sheath-like manner, but is also bonded physically and chemically to the plant polysaccharides. Unless the lignin is depolymerized, solubilized, or removed, the cellulose and hemicelluloses cannot be easily hydrolyzed by respective enzymes for their bioconversion into biofuels and chemicals. By now it has been established that lignin peroxidase (LiP) of white-rot fungus Phanerochaete chrysosporium is responsible for degradation of lignin. It has been reported that LiP is produced during secondary metabolism under carbon or nitrogen limitation by this organism. In literature, usually low yields (per unit volume) of LiP with P. chrysosporium have been reported. The reasons for low yields may be attributed to insufficient nitrogen in production media, which ultimately affects the synthesis of LiP protein. Therefore, it necessitated a search for an organism that can produce a ligninolytic enzyme system during its primary metabolism, without any effect of nitrogen limitation in the fermentation medium and without supply of extra oxygen to the cultures. Glenn and Gold were the first to report that decolorization of polymeric dyes in liquid cultures is related to the lignin degradation system. They demonstrated that like lignin degradation, the decolorization of polymeric dyes by the white-rot basidiomycete P. chrysosporium occurred during secondary metabolism, was suppressed in cultures grown in the presence of high levels of nitrogen, and was strongly dependent on the oxygen concentration in the cultures. The present study was undertaken to establish if certain dyes in solid media could be used to screen ligninolytic activity of selective actinomycetes during their primary metabolism without the limitation of nitrogen in the medium.

  5. Thrombin time and anti-IIa dabigatran's activity: hypothesis of thrombin time's predictive value.

    PubMed

    Le Guyader, Maïlys; Kaabar, Mohammed; Lemaire, Pierre; Pineau Vincent, Fabienne

    2015-01-01

    Dabigatran etexilate (Pradaxa®) is a new oral anticoagulant, competitive inhibitor, selective, fast, direct and reversible of thrombin. Dabigatran has an impact on a large panel of used coagulation tests. There is no relationship between thrombin time's lengthening and anti-IIa activity. This study defines thrombin time's predictive value, when its time is normal. The result of negative value is 97,6%. 255 patients were studied between January 2013 and July 2014. Thrombin time and anti-IIa activity were dosed for each patient. This study can be an assistant for therapeutic decision for laboratories without specialized test. PMID:26489812

  6. Screening of anti-bacterial activity of medicinal plants from Belize (Central America).

    PubMed

    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). PMID:12787962

  7. Real-time analysis of dual-display phage immobilization and autoantibody screening using quartz crystal microbalance with dissipation monitoring

    PubMed Central

    Rajaram, Kaushik; Losada-Pérez, Patricia; Vermeeren, Veronique; Hosseinkhani, Baharak; Wagner, Patrick; Somers, Veerle; Michiels, Luc

    2015-01-01

    Over the last three decades, phage display technology has been used for the display of target-specific biomarkers, peptides, antibodies, etc. Phage display-based assays are mostly limited to the phage ELISA, which is notorious for its high background signal and laborious methodology. These problems have been recently overcome by designing a dual-display phage with two different end functionalities, namely, streptavidin (STV)-binding protein at one end and a rheumatoid arthritis-specific autoantigenic target at the other end. Using this dual-display phage, a much higher sensitivity in screening specificities of autoantibodies in complex serum sample has been detected compared to single-display phage system on phage ELISA. Herein, we aimed to develop a novel, rapid, and sensitive dual-display phage to detect autoantibodies presence in serum samples using quartz crystal microbalance with dissipation monitoring as a sensing platform. The vertical functionalization of the phage over the STV-modified surfaces resulted in clear frequency and dissipation shifts revealing a well-defined viscoelastic signature. Screening for autoantibodies using antihuman IgG-modified surfaces and the dual-display phage with STV magnetic bead complexes allowed to isolate the target entities from complex mixtures and to achieve a large response as compared to negative control samples. This novel dual-display strategy can be a potential alternative to the time consuming phage ELISA protocols for the qualitative analysis of serum autoantibodies and can be taken as a departure point to ultimately achieve a point of care diagnostic system. PMID:26316752

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

    PubMed Central

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

    2016-01-01

    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. 1H 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. PMID:26905263

  9. Time Delay Evolution of Five Active Galactic Nuclei

    NASA Astrophysics Data System (ADS)

    Kovačević, A.; Popović, L. Č.; Shapovalova, A. I.; Ilić, D.; Burenkov, A. N.; Chavushyan, V. H.

    2015-12-01

    Here we investigate light curves of the continuum and emission lines of five type 1 active galactic nuclei (AGN) from our monitoring campaign, to test time-evolution of their time delays. Using both modeled and observed AGN light curves, we apply Gaussian kernel-based estimator to capture variation of local patterns of their time evolving delays. The largest variations of time delays of all objects occur in the period when continuum or emission lines luminosity is the highest. However, Gaussian kernel-based method shows instability in the case of NGC 5548, 3C 390.3, E1821 + 643 and NGC 4051 possibly due to numerical discrepancies between damped random walk (DRW) time scale of light curves and sliding time windows of the method. The temporal variations of time lags of Arp 102B can correspond to the real nature of the time lag evolution.

  10. The Contribution of Former Work-Related Activity Levels to Predict Physical Activity and Sedentary Time during Early Retirement: Moderating Role of Educational Level and Physical Functioning

    PubMed Central

    Van Dyck, Delfien; Cardon, Greet; Deforche, Benedicte; De Bourdeaudhuij, Ilse

    2015-01-01

    Background The transition to retirement introduces a decline in total physical activity and an increase in TV viewing time. Nonetheless, as more time becomes available, early retirement is an ideal stage to implement health interventions. Therefore, knowledge on specific determinants of physical activity and sedentary time is needed. Former work-related physical activity has been proposed as a potential determinant, but concrete evidence is lacking. The aim of this study was to examine if former work-related sitting, standing, walking or vigorous activities predict physical activity and sedentary time during early retirement. Additionally, moderating effects of educational level and physical functioning were examined. Methods In total, 392 recently retired Belgian adults (>6 months, <5 years) completed the International Physical Activity Questionnaire, the SF-36 Health Survey and a questionnaire on sociodemographics and former work-related activities. Generalized linear regression analyses were conducted in R. Moderating effects were examined by adding cross-products to the models. Results More former work-related sitting was predictive of more screen time during retirement. Lower levels of former work-related vigorous activities and higher levels of former work-related walking were associated with respectively more cycling for transport and more walking for transport during retirement. None of the predictors significantly explained passive transportation, cycling and walking for recreation, and leisure-time moderate-to-vigorous physical activity during retirement. Several moderating effects were found, but the direction of the interactions was not univocal. Conclusions Former-work related behaviors are of limited importance to explain physical activity during early retirement, so future studies should focus on other individual, social and environmental determinants. Nonetheless, adults who previously had a sedentary job had higher levels of screen time during

  11. Physician Activities During Time Out of the Examination Room

    PubMed Central

    Gilchrist, Valerie; McCord, Gary; Schrop, Susan Labuda; King, Bridget D.; McCormick, Kenelm F.; Oprandi, Allison M.; Selius, Brian A.; Cowher, Michael; Maheshwary, Rishi; Patel, Falguni; Shah, Ami; Tsai, Bonny; Zaharna, Mia

    2005-01-01

    PURPOSE Comprehensive medical care requires direct physician-patient contact, other office-based medical activities, and medical care outside of the office. This study was a systematic investigation of family physician office-based activities outside of the examination room. METHODS In the summer of 2000, 6 medical students directly observed and recorded the office-based activities of 27 northeastern Ohio community-based family physicians during 1 practice day. A checklist was used to record physician activity every 20 seconds outside of the examination room. Observation excluded medical care provided at other sites. Physicians were also asked to estimate how they spent their time on average and on the observed day. RESULTS The average office day was 8 hours 8 minutes. On average, 20.1 patients were seen and physicians spent 17.5 minutes per patient in direct contact time. Office-based time outside of the examination room averaged 3 hours 8 minutes or 39% of the office practice day; 61% of that time was spent in activities related to medical care. Charting (32.9 minutes per day) and dictating (23.4 minutes per day) were the most common medical activities. Physicians overestimated the time they spent in direct patient care and medical activities. None of the participating practices had electronic medical records. CONCLUSIONS If office-based, medically related activities were averaged over the number of patients seen in the office that day, the average office visit time per patient would increase by 7 minutes (40%). Care delivery extends beyond direct patient contact. Models of health care delivery need to recognize this component of care. PMID:16338912

  12. Trajectory data analyses for pedestrian space-time activity study.

    PubMed

    Qi, Feng; Du, Fei

    2013-01-01

    It is well recognized that human movement in the spatial and temporal dimensions has direct influence on disease transmission(1-3). An infectious disease typically spreads via contact between infected and susceptible individuals in their overlapped activity spaces. Therefore, daily mobility-activity information can be used as an indicator to measure exposures to risk factors of infection. However, a major difficulty and thus the reason for paucity of studies of infectious disease transmission at the micro scale arise from the lack of detailed individual mobility data. Previously in transportation and tourism research detailed space-time activity data often relied on the time-space diary technique, which requires subjects to actively record their activities in time and space. This is highly demanding for the participants and collaboration from the participants greatly affects the quality of data(4). Modern technologies such as GPS and mobile communications have m