Aryl 1,4-diazepane compounds as potent and selective CB2 agonists: optimization of drug-like properties and target independent parameters

A high throughput screening campaign identified aryl 1,4-diazepane compounds as potent and selective cannabinoid receptor 2 agonists as compared to cannabinoid receptor 1. This class of compounds suffered from poor drug-like parameters as well as low microsomal stability and poor solubility. Structure-activity relationships are described with a focus on improving the drug-like parameters resulting in compounds with improved solubility and permeability.     

光衰减及其相关环境因子对沉水植物生长影响研究进展

光衰减对沉水植物的生长具有至关重要的影响。系统归纳总结了光衰减及其相关环境因子对沉水植物生长的影响,指出:光因子是沉水植物生长的第一环境要素,水体中的有色可溶性有机质、浮游植物叶片细胞中的叶绿素和悬浮颗粒物以及水体本身,对光穿透水体时光强的衰减有着直接的影响,是影响沉水植物最重要的光衰减水质参数。其他环境因子如营养盐、沉积物和流水动力学等因素,则会直接或间接影响光衰减水质参数,进而影响水体透明度和浑浊度,影响沉水植物的光合作用,是影响沉水植物光衰减的间接环境因子。提出了研究中重点关注的几个问题。     

Demographic traits of Hippodamia variegata (Goeze) (Coleoptera: Coccinellidae) reared on Aphis fabae Scopoli (Hemiptera: Aphididae)

Lady beetles are the most important predatory species among arthropods; thus, studying their population parameters gives a clear picture about their life span. The demography of the lady beetle, Hippodamia variegata (Goeze) (Coleoptera: Coccinellidae), was studied under laboratory condition, on Aphis fabae at 27?°C based on the age-stage, two-sex life table. The means and standard errors were estimated by the bootstrap techniques. The results showed that the intrinsic rate of increase (r) and the finite rate of increase (λ) were 0.18 and 1.20 d^?1, respectively. The net reproduction rate (R ₀) and the gross reproduction rate were 232.49 and 442.48 offspring/individual, respectively. The mean generation time (T) was 29.03?days. The first peak of reproductive value in females was on the 18th day, which coincides with the total pre-oviposition period counted from birth. The life expectancy curve (e_xj ) of a new hatched female adult was 60?days. The results demonstrated that growth, survival and development of the predator can be described accurately by use of the age-stage, two-sex life table.     

Relationship between pollen emission and fruit production in olive (Olea europaea L.)

Aerobiological data of pollen emission concentrations is used to predict fruit production. The principal aim of this work was to study the relationship between pollen emission patterns, emission homogeneity and fruit production in olive (Olea europaea L.). Data of daily pollen concentrations in the atmosphere during the flowering period, collected over a 20‐year period in Perugia (Central Italy), and the corresponding fruit production data were analysed. Correlation and regression analyses on the partial pollen amounts (subdivisions of the whole flowering period), their statistical variability (expressed as coefficients of variation of the daily pollen concentration), and the production values in the different years demonstrate that pollen emission, during the seven to ten day period immediately preceding the maximum pollen emission day, appears to be most closely related to fruit production. Moreover, the pollen emission homogeneity (minimal variability in daily pollen concentrations) during the “critical” flowering period is very important for fertilization.     

Synthesis of Novel Alkyl Triphosphates and Their Substrate Properties Toward Terminal Deoxynucleotidyltransferase

Novel triphosphate derivatives bearing bulky or small groups at α-position attached to the triphosphate residue through linkers of different structures and lengths were synthesized and studied as substrates toward terminal deoxynucleotidyltransferase. The substrate efficacy depends on the structure of substituents, linker length, and nature of metal activator. The replacement of hydrophobic groups by small substituents decreased the substrate efficacy by about 20 times in respect to hydrophobic residues. The dependence on metal activator is the following: Co²⁺ > Mn²⁺ >> Mg²⁺. The model of interaction of alkyl triphosphates with linkers of different lengths bearing TdT active site is presented.     

Floristic composition and spatial distribution assessment of montane mesophilous grasslands in the central Apennines,Italy: A multi-scale and diachronic approach

Abstract

Evaluation of past land use offers valuable information in seeking to understand the distribution patterns of plant communities, insofar as such activity may have altered soil features, causing anthropogenic soil patchiness and marked plant diversity both locally and regionally. This study sought to provide a general overview of the relationships between the different syntaxonomical units and the soil features in a sub-Mediterranean grassland landscape, starting from assessment of soil parameters. In addition, we wanted to verify whether soil features and hierarchical landscape assessments of grasslands under homogeneous grazing disturbance are sufficient to explain the floristic differentiation of the plant communities, and whether study of land use history helps explain the distribution patterns of these plant communities. A clear understanding of the relationships between environmental factors and the floristic composition of plant communities is a strong basis for future inquiries into how disturbance variations (grazing, mowing, manuring, etc.) and past land use variations have affected grassland structures. This study examined nine syntaxa that develop on semi-flat slopes or those with northern exposure.     

Relation between climatic factors,diet and reproductive parameters of Little Terns over a decade

We used 10 years of data on clutch size, egg size and diet, and 8 years of data on timing of laying on Little Terns (Sternula albifrons) breeding in Ria Formosa lagoon system, Algarve, Portugal to assess whether diet acts as an important intermediary between climatic conditions and breeding parameters. We used Generalized Linear Models to relate (1) the relative occurrence and size of the main prey species, sand smelts (Atherina spp.), with environmental variables, a large-scale climate variable, the North Atlantic Oscillation (NAO) index, and a local scale variable, the sea-surface temperature (SST), and (2) the respective effects of sand smelts relative occurrence, NAO index and SST on Little Tern breeding parameters. The diet of Little Terns was dominated by sand smelts, with a frequency occurrence of over 60% in all years. The winter SST (February) was negatively associated with the relative occurrence of sand smelts in the diet of Little Terns during the breeding season which, in turn, was positively associated with Little Tern clutch size. Our results suggest that negative NAO conditions in the Atlantic Ocean, often associated with rougher sea conditions (greater vertical mixing, stronger winds and lower SST) were related with earlier breeding, and lower SST in the surroundings of the colony during winter–spring favour the abundance of prey fish for Little Terns as well as their reproductive parameters. Climate patterns at both large and local scales are likely to change in the future, which may have important implications for estuarine seabirds in Southern Europe.     

Chronic effect of erythromycin on substrate biodegradation kinetics of activated sludge

This study evaluated the chronic impact of erythromycin, a macrolide antibiotic, on microbial activities, mainly focusing on changes in process kinetics induced on substrate biodegradation and all related biochemical processes of microbial metabolism. Experiments involved two fill/draw reactors sustained at steady state at two different sludge ages of 10 and 2.0 days, fed with peptone mixture and continuous erythromycin dosing of 50 mg/L. Oxygen uptake rate profiles were generated in a series of parallel batch reactors seeded with biomass from fill/draw systems at selected periods of steady-state operation. Experimental data were evaluated by model calibration reflecting inhibitory effect on process kinetics: continuous erythromycin dosing inhibited microbial growth, reduced the rate of hydrolysis, blocked substrate storage and accelerated endogenous respiration. Adverse impact was mainly due to changes inflicted on the composition of microbial community. Interruption of erythromycin feeding resulted in partial recovery of microbial response. Sludge age affected the nature of inhibition, indicating different process kinetics for faster growing microbial community. Kinetic evaluation additionally revealed the toxic effect of erythromycin, which inactivated a fraction of biomass. Mass balance using oxygen uptake rate data also identified a stoichiometric impact, where a fraction of available substrate, although completely removed, could not be utilized in metabolic activities.     

Comparative kinetic study between moving bed biofilm reactor-membrane bioreactor and membrane bioreactor systems and their influence on organic matter and nutrients removal

New technologies regarding wastewater treatment have been developed. Among these technologies, the moving bed biofilm reactor combined with membrane bioreactor (MBBR-MBR) is a recent solution alternative to conventional processes. This paper presents the results obtained from three wastewater treatment plants working in parallel. The first wastewater treatment plant consisted of a membrane bioreactor (MBR), the second one was a MBBR-MBR system containing carriers both in anoxic and aerobic zones, and the last one consisted of a MBBR-MBR system which contained carriers only in the aerobic zone. The reactors operated with a hydraulic retention time of 26.47 h. During the study, the difference between the experimental plants was not statistically significant concerning organic matter and nutrients removal. However, different tendencies regarding nutrients removal are shown by the three wastewater treatment plants. In this sense, the performances in terms of nitrogen and phosphorus removal of the MBBR-MBR system which contained carriers only in the aerobic zone (67.34 ± 11.22% and 50.65 ± 11.13%, respectively) were slightly better than those obtained from another experimental plants. As a whole, the pilot plant which consisted of a MBR showed better performance from the point of view of the kinetics of the heterotrophic and autotrophic biomass with values of μ_m,H = 0.00858 h⁻¹, μ_m,A = 0.07646 h⁻¹, K_M = 2.37 mg O₂ L⁻¹ and K_NH = 1.31 mg N L⁻¹.