Preliminary Structure-Activity Relationship on Theonellasterol, a New Chemotype of FXR Antagonist, from the Marine Sponge Theonella swinhoei

Using theonellasterol as a novel FXR antagonist hit, we prepared a series of semi-synthetic derivatives in order to gain insight into the structural requirements for exhibiting antagonistic activity. These derivatives are characterized by modification at the exocyclic carbon-carbon double bond at C-4 and at the hydroxyl group at C-3 and were prepared from theonellasterol using simple reactions. Pharmacological investigation showed that the introduction of a hydroxyl group at C-4 as well as the oxidation at C-3 with or without concomitant modification at the exomethylene functionality preserve the ability of theonellasterol to inhibit FXR transactivation caused by CDCA. Docking analysis showed that the placement of these molecules in the FXR-LBD is well stabilized when on ring A functional groups, able to form hydrogen bonds and π interactions, are present.     

From Farmers to Loggers: The Role of Shifting Cultivation Landscapes in Timber Production in Cameroon

This article focuses on timber sourced from the agricultural areas in the shifting cultivation landscapes of the Central Region of Cameroon. Data about volumes marketed in urban centres, harvesting operations and on-farm timber management are used to discuss the ecological impact of small-scale logging and its sustainability in the long term. An opportunistic association exists between small-scale logging and agricultural land uses, determined mostly by the abundance of valuable species in fallows and on cocoa farms, their easy accessibility and the low price of farmland timber. Farmers apply various strategies to the management of tree resources in fallows and cocoa agroforests, with most felling authorized in fallows and most trees preserved on the cocoa farms. With current agricultural expansion and intensification trends associated with small-scale logging, timber resources on rural land are at risk of depletion with direct consequences for domestic timber supply and the thousands of livelihoods it sustains. Marketing and regulatory changes are needed to encourage the integration of timber production in agricultural management systems.     

Cannabinoid receptors are widely expressed in goldfish: molecular cloning of a CB2-like receptor and evaluation of CB1 and CB2 mRNA expression profiles in different organs

Cannabinoids, the bioactive constituents of Cannabis sativa, and endocannabinoids, among which the most important are anandamide and 2-arachidonoylglycerol, control various biological processes by binding to specific G protein-coupled receptors, namely CB1 and CB2 cannabinoid receptors. While a vast amount of information on the mammalian endocannabinoid system does exist, few data have been reported on bony fish. In the goldfish, Carassius auratus, the CB1 receptor has been cloned and its distribution has been analyzed in the retina, brain and gonads, while CB2 had not yet been isolated. In the present paper, we cloned the goldfish CB2 receptor and show that it presents a quite high degree of amino acid identity with zebrafish Danio rerio CB2A and CB2B receptors, while the percentage of identity is lower with the puffer fish Fugu rubripes CB2, as also confirmed by the phylogenetic analysis. The sequence identity becomes much lower when comparing the goldfish and the mammalian CB2 sequences; as for other species, goldfish CB2 and CB1 amino acid sequences share moderate levels of identity. Western-blotting analysis shows the CB2 receptor as two major bands of about 53 and 40 kDa and other faint bands with apparent molecular masses around 70, 57 and 55 kDa. Since the distribution of a receptor could give information on its physiological role, we evaluated and compared CB1 and CB2 mRNA expression in different goldfish organs by means of qReal-Time PCR. Our results show that both CB1 and CB2 receptors are widely expressed in the goldfish, displaying some tissue specificities, thus opening the way for further functional studies on bony fish and other nonmammalian vertebrates.     

Occurrence, distribution, and role in abortion of Coxiella burnetii in sheep and goats in Sardinia, Italy

Between 1999 and 2002, 9349 sera and 517 aborted samples (422 foetuses and 95 placenta) were analysed from 675 sheep and 82 goat farms distributed all over the island of Sardinia. After abortion notification, sera collected at random from adult animals were examined to detect antibodies specific to Coxiella burnetii by ELISA, whereas foetuses and placenta were analysed by PCR assay. Specific IgG antibodies were detected in 255 (38%) sheep farms and in 39 (47%) goat herds whereas 40 ovine (10%) and 3 (6%) caprine foetuses were C. burnetii PCR-positive. Although C. burnetii DNA was amplified from different types of tissues, placenta was the tissue with the highest detection rate. Seroprevalence analysis indicates that C. burnetii distribution in sheep and goats is very high, but PCR results demonstrate that C. burnetii has a relatively low role in abortion, especially in goats.     

Effects of conventionally bred and <Emphasis Type="BoldItalic">Bacillus thuringiensis</Emphasis> (<Emphasis Type="BoldItalic">Bt</Emphasis>) maize varieties on soil microbial biomass and activity

Genetically modified (GM) maize containing genes from the soil bacterium Bacillus thuringiensis (Bt) was cultivated on 29% of the total maize production area worldwide in 2009. Most studies to date compare Bt-maize varieties with their near isogenic lines; however, there is little information on the variability of conventional maize breeding lines and how the effects of Bt varieties are ranked within. In our study on the potential risks of Bt-maize varieties, we analyzed tissue quality and compared the effects of ten conventional and GM maize varieties on soil microbiological properties in a replicated climate chamber experiment. All maize varieties were cultivated twice in the same soil microcosm. Shoot yields and soluble C in leaf tissue of Bt varieties were higher than the ones of non-Bt. Soil dehydrogenase activity was reduced by 5% under Bt varieties compared to non-Bt, while most of the other soil microbial properties (soil microbial biomass, basal respiration) showed no significant differences between Bt and non-Bt varieties. The leaves and roots of one Bt variety were decomposed to a greater extent than the ones of its near isogenic line; the conventional breeding lines also showed higher values. Changes in crop and soil parameters were found when comparing the first and the second crops, but the effects of repeated cropping were the same for all tested varieties. For the studied parameters, the variation among non-Bt-maize varieties was similar to the difference between Bt and non-Bt varieties.     

Studies on the transovarial transmission of Borrelia burgdorferi sensu lato in the taiga tick Ixodes persulcatus

The possibility of vertical transmission of Borrelia burgdorferi sensu lato in Ixodes persulcatus Schulze, 1930 ticks was studied in the progeny of 20 females collected from the vegetation in an active focus of ixodid tick-borne borrelioses (ITBB) located in the Perm oblast, Russia, where Borrelia garinii and B. afzelii are circulating. The presence of Borrelia DNA was detected by the PCR method after feeding and egg laying in 16 engorged females (80.0%), as well as in 36.5 +/- 7.2% samples containing 20 eggs each and in 21.4 +/- 4.2% samples containing 10 eggs each. The respective rates of individual egg infection were 0.4-8.0% and 0.5-23.0%. PCR analysis of 370 eggs (one egg per sample) and 781 unfed larvae hatched from the same egg masses (1, 10, 20, 40, and 50 larvae per sample) failed to reveal the presence of Borrelia DNA. Negative results were also obtained in experiments on inoculating the BSK II medium with the egg and larval materials. Microscopic analysis of 1,683 smear preparations of eggs and 1,416 preparations of unfed daughter larvae revealed spirochete-like cells in 7 (0.4 +/- 0.3%) and 13 (0.9 +/- 0.5%) preparations, respectively; typical Borrelia cells were found in seven preparations of larvae (0.5 +/- 0.4%). Only 1 out of 16 infected females transmitted Borrelia vertically, through the eggs to the larval progeny. The infection rate in this progeny was about 7%, and the prevalence of Borrelia in individual larvae was 0.4-0.8 cells per 100 microscopic fields. These data do not allow the conclusion that transovarial transmission of B. burgdorferi sensu lato in the I. persulcatus tick is an established fact. However, they show that, even if such transmission is possible, its probability is very low.     

GIS-models work well, but are not enough: Habitat preferences of Lanius collurio at multiple levels and conservation implications

Species conservation largely depends on knowledge of habitat needs of target species. GIS-models are increasingly used to assess habitat preferences and distribution of target species, but their accuracy is constrained by availability of digital data layers. We developed a two-steps approach aiming at showing pros and cons of landscape (GIS)- and site-level habitat models, identifying key habitat factors for conservation of a threatened bird species, the red-backed shrike Lanius collurio. A spatially explicit GIS-model was generated using landscape variables, and a second model at site level was developed using fine-scale variables measured on the ground. The GIS-based model was then extrapolated to the entire region to obtain a map of distribution of suitable habitats. Positive associations between shrike occurrence and both hedgerow length and partial shrub cover were detected at both scales. Shrikes were also positively associated with grassland cover at landscape level and with partial cover of untilled herbaceous vegetation at the finer scale, and negatively affected by lucerne cover. The GIS-model led to an affordable map of predicted habitat suitability which should help conservationists to focus on different local priorities, but was unable to identify effects of untilled and lucerne cover. Site-level model gave fine details for habitat management, but its application elsewhere requires ground-measurements of factors. Combining the multiscale models could indicate more urgent actions at large scales (e.g. maintaining suitable habitats, or improving connectivity among isolated patches) and draw a detailed figure of the most suitable habitat for the species. Shrike occurrence was associated with a higher number of shrub and tree species: the indicator value of the species should ensure general benefits for biodiversity from dedicated management.     

Effect of a hay-based diet or different upland grazing systems on milk volatile compounds

The effect of animal feeding on milk volatile organic compounds (VOCs) of metabolic origin was tested on a hay-based diet (H), a highly diversified pasture under continuous grazing (CG), or a less diversified pasture under rotational grazing (RG). Individual milk of 24 Montbe?liarde cows (8 per treatment) were sampled after 2 weeks. Pasture-derived milk was richer (p < 0.05) in camphene, sabinene, β-caryophyllene, and skatole than H milk. Neither milk yield nor fat content affected the majority of VOCs measured. Skatole increased slightly with milk yield, while indole and cineole decreased slightly with milk fat content but with poor regression (R(2) < 0.54). Multivariate analysis showed that, on the basis of those VOCs of metabolic origin whose concentration differed between treatment (dimethyl-sulfone, skatole, toluene, undecanoic acid, 1-octadecene, benzeneacetaldehyde, octanoic acid, and 2-pentanone-4-hydroxy-4-methyl), it was possible to obtain good discriminations among feeding systems. This study is promising for a future use of VOCs of metabolic origin to trace animal feeding systems.