Synthetic pyrazole derivatives as growth inhibitors of some phytopathogenic fungi

The present study was carried out to investigate the antifungal activity of pyrazole/isoxazole-3-carboxamido-4-carboxylic acids, 4-oxo-5-substituted pyrazolo[3,4-d]pyrimidine-6-thiones, and N-alkyl/aryl-N'-(4-carbethoxy-3-pyrazolyl)thioureas against Pythium ultimum, Botrytis cinerea, and Magnaporthe grisea. The results on growth inhibition showed differences in the sensitivity of the three fungi to the tested substances, and in general P. ultimum was shown to be the most sensitive. On all phytopathogens the best results within the pyrazole/isoxazolecarboxamide series are given by the compounds with the carboxamide and carboxylic groups in positions 3 and 4; the presence of these groups seems to be critical for biological activity in this series of compounds. Among the pyrazolopyrimidines the derivative supplied with the benzylic group was the most active on the three fungi and in particular against P. ultimum. Several compounds belonging to the thiourea series are able to inhibit selectively M. grisea at 50 and 10 microg mL(-1), doses at which the reference commercial compound tricyclazole had low or no effect.     

Synthesis of pyrazole derivatives and their evaluation as photosynthetic electron transport inhibitors

Two series of new pyrazoles, namely six pyrazolo[1,5-a][1,3,5]triazine-2,4-dione and four pyrazolo[1,5-c][1,3,5]thiadiazine-2-one derivatives, were synthesized as potential inhibitors of the photosynthetic electron transport chain at the photosystem II level. The compounds were confirmed by 1H NMR, elemental, and IR analyses. Their biological activity was evaluated in vivo upon both the growth of blue-green algae and the photosynthetic oxygen evolution by eukaryotic algae and in vitro as the ability to interfere with light-driven reduction of ferricyanide by isolated spinach chloroplasts. Some compounds exhibited remarkable inhibitory properties, comparable to those of the reference commercial herbicides lenacil, diuron, and hexazinone. Results suggest that the substitution of triazine with thiadiazine ring may act as amplifier for herbicidal activity.     

Direct antioxidant activity of purified glucoerucin, the dietary secondary metabolite contained in rocket (Eruca sativa Mill.) seeds and sprouts

Rocket (Eruca sativa Mill. or Eruca vesicaria L.) is widely distributed all over the world and is usually consumed fresh (leafs or sprouts) for its typical spicy taste. Nevertheless, it is mentioned in traditional pharmacopoeia and ancient literature for several therapeutic properties, and it does contain a number of health promoting agents including carotenoids, vitamin C, fibers, flavonoids, and glucosinolates (GLs). The latter phytochemicals have recently gained attention as being the precursors of isothiocyanates (ITCs), which are released by myrosinase hydrolysis during cutting, chewing, or processing of the vegetable. ITCs are recognized as potent inducers of phase II enzymes (e.g., glutathione transferases, NAD(P)H:quinone reductase, epoxide hydrolase, etc.), which are important in the detoxification of electrophiles and protection against oxidative stress. The major GL found in rocket seeds is glucoerucin, GER (108 +/- 5 micromol g(-)(1) d.w.) that represents 95% of total GLs. The content is largely conserved in sprouts (79% of total GLs), and GER is still present to some extent in adult leaves. Unlike other GLs (e.g., glucoraphanin, the bio-precursor of sulforaphane), GER possesses good direct as well as indirect antioxidant activity. GER (and its metabolite erucin, ERN) effectively decomposes hydrogen peroxide and alkyl hydroperoxides with second-order rate constants of k(2) = 6.9 +/- 0.1 x 10(-)(2) M(-)(1) s(-)(1) and 4.5 +/- 0.2 x 10(-)(3) M(-)(1) s(-) , respectively, in water at 37 degrees C, thereby acting as a peroxide-scavenging preventive antioxidant. Interestingly, upon removal of H(2)O(2) or hydroperoxides, ERN is converted into sulforaphane, the most effective inducer of phase II enzymes among ITCs. On the other hand, ERN (and conceivably GER), like other ITCs, does not possess any chain-breaking antioxidant activity, being unable to protect styrene from its thermally (37 degrees C) initiated autoxidation in the presence of AMVN. The mechanism and relevance of the antioxidant activity of GER and ERN are discussed.     

Pharmacokinetics of injectable marbofloxacin after intravenous and intramuscular administration in red-eared sliders (Trachemys scripta elegans)

Fluoroquinolone antibacterial drugs are currently used in reptilian medicine because of their broad spectrum of activity including the most frequent pathogens of these species. The disposition kinetics of marbofloxacin (MBX) at a single dose of 2 mg/kg were determined in healthy red-eared sliders after intravenous (IV) and intramuscular (IM) administration. The influence of renal portal system on the bioavailability of the drug was investigated by using forelimb and hindlimb as IM injection sites. Apparent volume of distribution at steady-state (V_ss) and systemic clearance (Cl) of marbofloxacin after IV administration were estimated to be 48.21 ± 5.42 ml/kg and 23.38 ± 2.90 ml/hr·kg, respectively. The absolute bioavailabilities after IM route were 45.96% (forelimb) and 52.09% (hindlimb). The lack of statistically significant differences in most of the pharmacokinetic parameters after the two IM injection sites suggests a negligible influence of renal portal system in clinical use of MBX, although the C_max after IM_fore administration is advantageous, having into account the concentration-dependent action of this antibiotic. The absence of visible adverse reactions in the animals and the advantageous pharmacokinetic properties suggest the possibility of its safe and effective clinical use in red-eared sliders.     

Optimizing fen peatland water-table depth for romaine lettuce growth to reduce peat wastage under future climate warming

Forty percentage of UK peatlands have been drained for agricultural use, which has caused serious peat wastage and associated greenhouse gas emissions (carbon dioxide (CO₂) and methane (CH₄)). In this study, we evaluated potential trade-offs between water-table management practices for minimizing peat wastage and greenhouse gas emissions, while seeking to sustain romaine lettuce production: one of the most economically relevant crop in the East Anglian Fenlands. In a controlled environment experiment, we measured lettuce yield, CO_2, CH₄ fluxes and dissolved organic carbon (DOC) released from an agricultural fen soil at two temperatures (ambient and +2°C) and three water-table levels (−30 cm, −40 cm and −50 cm below the surface). We showed that increasing the water table from the currently used field level of −50 cm to −40 cm and −30 cm reduced CO₂ emissions, did not affect CH₄ fluxes, but significantly reduced yield and increased DOC leaching. Warming of 2°C increased both lettuce yield (fresh leaf biomass) and peat decomposition through the loss of carbon as CO₂ and DOC. However, there was no difference in the dry leaf biomass between the intermediate (−40 cm) and the low (−50 cm) water table, suggesting that romaine lettuce grown at this higher water level should have similar energetic value as the crop cultivated at −50 cm, representing a possible compromise to decrease peat oxidation and maintain agricultural production.     

Different mechanisms control lipoxygenase activity in durum wheat kernels

Yellow pigment content (YPC), lipoxygenase (LPX) activity and the polymorphism at the Lpx-B1.1 locus were assessed on an Italian durum wheat germplasm collection and four varieties contrasting for YPC and LPX activity were then characterized in terms of Lpx gene expression, biochemical LPX properties and their performance during pasta processing. The screening of 71 genotypes showed a great genetic variability for YPC (3.68–9.43 μg/g dw) and LPX activity (0.02–7.91 EU/g dw). The Lpx-B1.1 polymorphism was significantly associated with differences in LPX activity. Besides the Lpx-B1.1 deletion, different expression levels of Lpx mRNAs were found associated with differences in LPX activity. The temporal expression of three Lpx genes showed different profiles among the cultivars investigated. Genotypes with high LPX activity showed an anticipated temporal expression for Lpx-1 compared to low LPX activity ones. The LPX activity in the analysed genotypes is most likely due to the contribution of different LPX isoforms observed in the later stage of grain filling.     

Current research on the use of plant‐derived products in farmed fish

Over the years, aquaculture has shown increasing development in terms of production. However, due to intensive farming practices, infectious diseases represent the main problem in fish farms, causing heavy economic losses. The use of antibiotics for controlling diseases is widely criticized for its negative impact, including selection of antibiotic‐resistant bacterial strains, immunosuppression, environmental pollution and accumulation of chemical residues in fish tissues. On the other hand, though vaccination is the most effective prophylactic method of preventing disease outbreaks, the development of effective formulations is often hindered by high production costs and the antigenic heterogeneity of the microbial strains. Recently, there has been increased interest in the possibility of using medicinal herbs as immunostimulants, capable of enhancing immune responses and disease resistance of cultured fish. Plant‐derived products seem to represent a promising source of bioactive molecules, being at the same time readily available, inexpensive and biocompatible. The aim of this article is to provide an overview of recent research dealing with the use of medicinal plants in aquaculture. Special attention is given to the information about the effects of plant extracts/products on fish growth, haematological profiles, immune responses and resistance to infectious diseases.     

Assessment of the impact of forest harvesting operations on the physical parameters and microbiological components on a Mediterranean sandy soil in an Italian stone pine stand

Forest harvesting operations may have a significant impact on soil physical properties by reducing its porosity and organic functions. Soil variations, in particular bulk density and total porosity, caused by external perturbations as soil becomes compacted due to machinery passes, can lead to changes in biogeochemical cycles that have consequences on soil ecosystems. This study investigated how the impact of forest operations and the elapsed time from harvest can influence: (1) the physical–chemical characteristics of soil and (2) the nitrogen-fixing and nitrifying microbial communities. The study area is located inside the Regional Park of Migliarino, San Rossore, Massaciuccoli (Pisa, Italy). In the study area, the soil has been classified as recent sands with sandy loam texture and slightly calcareous (USDA Soil Taxonomy classification). Soil samples were collected in patchy cut areas (strip cut) of Pinus pinea stand that was harvested in two steps: half area in 2006 and the rest in 2011. Soil samples were collected also in a control area (not harvested) with similar stand and soil characteristics. Statistical analysis was preceded by a test of normality (Kolmogorov–Smirnov test) and a variance homogeneity test (Levene’s test). Considering the dependence of the variables studied (physical and chemical soil characteristics), a MANOVA test and a post hoc Tukey HSD test were applied to determine statistical difference among the three treatments: harvested 2006, harvested 2011 and not harvested. The results did not indicate significant variations to the parameters of shear and penetration resistance, though soil bulk density and total porosity were significantly altered in the short period since forestry operations occurred. These physical changes induced qualitative (presence/absence and number of species) and quantitative (abundance and spatial evenness of the species) variations in the nitrogen-fixing and nitrifying microbial communities.     

Association of microalbuminuria and the urine albumin-to-creatinine ratio with systemic disease in cats

OBJECTIVE: To determine the diagnostic usefulness of semiquantitative and quantitative microalbuminuria assays and urine albumin-to-creatinine (UAC) ratio for detecting disease in cats. DESIGN: Prospective study. ANIMALS: 441 cats evaluated at a veterinary teaching hospital. PROCEDURES: Urine samples from cats for which a complete medical record was available were included. Urine dipstick results, urine protein-to-creatinine ratios (cutoffs, 0.1 and 0.4), semiquantitative and quantitative microalbuminuria assay results (cutoff, 1 mg/dL), and UAC ratio values (cutoffs, 100 and 200 mg/g) were determined. Clinical diagnoses determined within 3 months of enrollment were recorded. Sensitivity and specificity were determined with disease status used as the standard. The influences of clinical diagnosis, sex, age, serum urea nitrogen and creatinine concentrations, blood pressure, bacterial urine culture results, rectal temperature, pyuria, hematuria, and bacteriuria were evaluated by means of logistic regression. RESULTS: Of 441 cats that were eligible for inclusion, 40 were healthy and 401 had > or = 1 disease. Results of logistic regression indicated that significant associations existed for age, presence of disease, presence of urinary tract disease, azotemia, hematuria, and pyuria and results of 1 or both of the microalbuminuria assays. CONCLUSIONS and CLINICAL RELEVANCE: Microalbuminuria was associated with underlying disease. Sensitivity and specificity of the microalbuminuria assays for detection of systemic disease were superior to those of other tests. Microalbuminuria testing in conjunction with other screening procedures may increase identification of occult disease. A prospective study evaluating the predictive values of screening tests with and without microalbuminuria determination is needed to validate this recommendation.