Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators

A series of dihydro-9,10-ethano-anthracene-11-carboxamides as novel glucocorticoid receptor modulators is reported. SAR exploration identified compounds from this series displaying a promising dissociation profile in discriminating between transrepression and transactivation activities. 17a is a partial agonist of GR-mediated transactivation which elicits potent and efficacious transrepression in reporter gene assays. A hypothetical binding mode is provided which accounts for the induction of functional activity by a bridgehead methyl group.     

Correlates of Unintended Pregnancy in Ethiopia: Results From a National Survey

Background

Unintended pregnancy has been a major reproductive health challenge in resource poor settings including Ethiopia. It has adverse consequences to the mother, child and the health sector’s resources. Understanding the extent of unintended pregnancy and the factors associated is crucial to devise evidence based interventions. The analysis was aimed at assessing the unintended pregnancy prevalence rate among pregnant women and the factors predisposing to unintended pregnancy.

Methods

This secondary data analysis was done on women’s dataset from the 2011 Ethiopian Demographic and Health Survey (DHS). A total of 1267 pregnant women were included in the analysis. Multiple logistic regression analysis was performed using SPSS software to identify the factors associated with unintended pregnancy. Odds Ratio with 95% confidence interval (95% CI) was computed to assess the association of different factors with unintended pregnancy.

Results

The overall prevalence of unintended pregnancy was found to be 24%: those who wanted it at a later time and not at all accounted for 17.1% and 6.9%, respectively. The unintended pregnancy rate ranged from 1.5% in Afar Regional State to 39.8% in Oromiya Regional State. Women who knew the timing of ovulation had a 45% reduced chance of unintended pregnancy (OR (95% CI): 0.55 (0.35, 0.85)). Ever use of family planning, presence of five or more born children, and two or more births in the past five years were associated with unintended pregnancy (OR (95% CI): 1.79 (1.31, 2.45), 2.36 (1.01, 5.49) and 2.00 (1.12, 3.58), respectively).

Conclusions

A significant proportion of the current pregnancies were found to be unintended with significant variations among the different regions. Women already burdened with higher fertility were suffering from unintended pregnancy. Family planning programs need to concentrate on the highly affected regions and target women with higher fertility to reduce the level of unintended pregnancy at national level.     

Development of vesicular-arbuscular mycorrhizal infection and the uptake of immobile nutrients inLeucaena leucocephala

The level of vesicular-arbuscular mycorrhizal (VAM) infection in the roots of Leucaena grown in a sand-soil mixture in the greenhouse increased rapidly with time and reached a peak value of 84% at 30 days from planting. The pattern of immobile nutrient uptake and accumulation closely paralleled that of the development of infection, particularly during the first 10–30 days after planting. Significant changes in dry matter yield were also observed only after a significant portion of the root length was colonized byGlomus aggregatum. The development of VAM infection was not accompanied by growth depression at any of the sampling periods. However, VAM roots had very high levels of Cu which was not translocated to shoots. It is hypothesized that such a diversion of Cu by the endophyte from the host could cause growth depression under conditions where the soil volume is supplied with sub-optimal levels of Cu. Contribution from the Hawaii Institute of Tropical Agriculture and Human Resources Series No. 3186.     

Nitrogen Fixation by Photosynthetic Bacteria in Lowland Rice Culture

Propanil (3′,4′-dichloropropionanilide) was a potent inhibitor of the nitrogenase activity of blue-green algae (cyanobacteria) in flooded soil, but the herbicide at comparable concentrations was not toxic to rice, protozoa, and nitrogen-fixing bacteria. Ethanol-amended flooded soils treated with propanil exhibited higher rates of nitrogenase activity than those not treated with the herbicide. The enhanced nitrogenase activity in propanil-treated soils was associated with a rise in the population of purple sulfur bacteria, especially of cells resembling Chromatium and Thiospirillum. By employing propanil and a means of excluding light from the floodwater to prevent the development of phototrophs during rice growth under lowland conditions, the relative activities of blue-green algae, photosynthetic bacteria, and the rhizosphere microflora were determined. The results suggest that the potential contribution of photosynthetic bacteria may be quite high.     

Response of Sesbania grandiflora to Inoculation of Soil with Vesicular-Arbuscular Mycorrhizal Fungi

A greenhouse experiment was conducted to determine the influence of two tropical isolates of Glomus fasciculatum and Glomus mosseae on the nutrient uptake and growth of Sesbania grandiflora. Inoculation of sterile soil with the fungi significantly improved growth and nutrient uptake by S. grandiflora, but the response of the legume was markedly better when the soil was inoculated with G. fasciculatum than when it was inoculated with G. mosseae. Nutrient uptake and growth of S. grandiflora in nonsterile soil was also significantly stimulated by inoculation, but the legume did not respond differently to the two endophytes under this condition.     

Welternährung im 21. Jahrhundert. Eine umfassende Herausforderung (Teil 1)

Nutrition of the world's population in the 21st century often appears as an unsolved problem. The challenges are bigger than an increase in agricultural production. From a brief review on the history of food production diverse aspects of the development become evident: innovations with their beneficial and non‐beneficial aspects, e.g. the, green revolution' increasing the rice yields on one hand and the number of landless people on the other. Great differences can be found in agricultural productivity: the yields of the presently area under the plough can be increased. Climate change impacts on the framework of agricultural production with losses and gains of arable land. The challenges of global nutrition cannot be met by innovations in plant breeding and cultivation alone. Socioeconomic factors, education, and health become increasingly important.     

Traffic Noise and Inequality in the Twin Cities,Minnesota

It is widely known that prolonged exposure to high levels of traffic noise has several health effects. While scholarship in environmental justice has explored the environmental equity hypothesis in a wide range of areas, whether the spatial distribution of traffic noise is equitable among different racial and socioeconomic groups has rarely been explored, especially in the United States. This article addresses this lacuna by examining this relationship in the Twin Cities Metro Region, Minnesota. Traffic data from the Minnesota Department of Transportation were used to model the propagation of traffic noise over the study area and aircraft noise contour lines were added to account for aircraft noise. Inequities associated with exposure to chronic traffic noise were investigated using selected demographic and socioeconomic variables from the U.S. Census 2000. Statistical analysis was based on a regression model that addressed spatial autocorrelation. Results indicate that there is an association between noise levels and household income, median household value, the percentage of non-white residents, and the percentage of the population less than 18 years of age.     

Structural Characterization of HIV gp41 with the Membrane-proximal External Region

Human immunodeficiency virus, type 1 (HIV-1) envelope glycoprotein (gp120/gp41) plays a critical role in virus infection and pathogenesis. Three of the six monoclonal antibodies considered to have broadly neutralizing activities (2F5, 4E10, and Z13e1) bind to the membrane-proximal external region (MPER) of gp41. This makes the MPER a desirable template for developing immunogens that can elicit antibodies with properties similar to these monoclonal antibodies, with a long term goal of developing antigens that could serve as novel HIV vaccines. In order to provide a structural basis for rational antigen design, an MPER construct, HR1-54Q, was generated for x-ray crystallographic and x-ray footprinting studies to provide both high resolution atomic coordinates and verification of the solution state of the antigen, respectively. The crystal structure of HR1-54Q reveals a trimeric, coiled-coil six-helical bundle, which probably represents a postfusion form of gp41. The MPER portion extends from HR2 in continuation of a slightly bent long helix and is relatively flexible. The structures observed for the 2F5 and 4E10 epitopes agree well with existing structural data, and enzyme-linked immunosorbent assays indicate that the antigen binds well to antibodies that recognize the above epitopes. Hydroxyl radical-mediated protein footprinting of the antigen in solution reveals specifically protected and accessible regions consistent with the predictions based on the trimeric structure from the crystallographic data. Overall, the HR1-54Q antigen, as characterized by crystallography and footprinting, represents a postfusion, trimeric form of HIV gp41, and its structure provides a rational basis for gp41 antigen design suitable for HIV vaccine development.     

Welternährung im 21. Jahrhundert. Eine umfassende Herausforderung (Teil 2)

In the 21st century global nutrition security does not necessarily become an unsolvable challenge. Besides changes in agricultural production securing food availability should become the first priority. The overall aim is to overcome nutrition insecurity and to promote a healthy diet for all human beings. The biggest obstacle for the process of attaining global nutrition security are the present global economic and trade relations. Education, health care and promotion of equal gender relations can help to improve the situation in developing countries. The natural ressources are sufficient to meet the goal of nutrition and food security of the growing global population if they are used for the benefit of consumers giving due consideration to environmental protection.     

Effect of Rice Plants on Nitrogenase Activity of Flooded Soils

In samples of flooded soil containing blue-green algae (cyanobacteria), the presence of rice plants did not influence the nitrogenase activity of the algae. Nitrogenase activity of heterotrophic bacteria was enhanced by the presence of rice plants, but this activity was not affected by changes in plant density. The rate of nitrogen fixation in the rhizosphere, however, varied significantly among the 16 rice varieties tested. A simple method was devised to test the nitrogen-fixing activity in the root zone of rice varieties, and data were obtained showing marked differences in the activities of the 16 varieties. In tests of two varieties with dissimilar rates of nitrogen fixation in their rhizospheres, the variety which had the greater root weight and lesser shoot weight and which supported greater methane formation had the greater nitrogenase activity.