Dual Targeting of PTP1B and Aldose Reductase with Marine Drug Phosphoeleganin: A Promising Strategy for Treatment of Type 2 Diabetes

An in-depth study on the inhibitory mechanism on protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AR) enzymes, including analysis of the insulin signalling pathway, of phosphoeleganin, a marine-derived phosphorylated polyketide, was achieved. Phosphoeleganin was demonstrated to inhibit both enzymes, acting respectively as a pure non-competitive inhibitor of PTP1B and a mixed-type inhibitor of AR. In addition, in silico docking analyses to evaluate the interaction mode of phosphoeleganin with both enzymes were performed. Interestingly, this study showed that phosphoeleganin is the first example of a dual inhibitor polyketide extracted from a marine invertebrate, and it could be used as a versatile scaffold structure for the synthesis of new designed multiple ligands.     

A study of gross,histological and blood biochemical changes in rainbow trout,Oncorhynchus mykiss (Walbaum), with rainbow trout gastroenteritis (RTGE)

The mechanisms behind the pathogenesis of rainbow trout gastroenteritis (RTGE) are still unknown. This study examined the macroscopic and microscopic changes in trout with RTGE (RTGE+), as well as the blood chemistry. A total of 464 rainbow trout were sampled from 11 sites in the UK, comprising 152 RTGE+ fish and 330 random, apparently healthy fish. A case definition for RTGE was assessed by the analysis of its agreement with three laboratory tests: histopathology, packed cell volume and kidney bacteriology. Cluster analysis indicated the presence of three distinct presentations within the population of RTGE+ fish. Cluster A included gross signs associated with moribund RTGE+ fish, and clusters B and C identified gross signs consistent with concurrent diseases, notably furunculosis, enteric redmouth and proliferative kidney disease. The information gained was used to select RTGE+ fish without concurrent disease for the analysis of RTGE pathogenesis with blood biochemistry. This analysis revealed a severe osmotic imbalance and a reduced albumin/globulin ratio as indicatives of selective loss of albumin. These findings are compatible with a protein losing enteropathy.     

The Biochemical Composition of Chaetoceros muelleri (Lemmermann Grown) with an Agricultural Fertilizer

The aim of this work was to demonstrate that the source of nitrogen of microalgae growth media has an effect on the biochemical composition by comparing the composition of Chaetoceros muelleri grown in semicontinuous cultures with 30% daily dilutions with an agricultural fertilizer containing three nitrogen sources (AF) and with the traditional f/2 medium. The cell yields, proximate composition, and total essential and nonessential amino acid contents of C. muelleri were similar, but phenylalanine and glutamate were significantly higher with f/2, and alanine was higher with AF. Monounsaturated fatty acids were higher in AF‐grown cultures, but polyunsaturates were higher with f/2. Among polyunsaturates, 20:5n‐3 (eicosapentaenoic acid, EPA) was higher with AF (17.16%) than with f/2 (13.44%), whereas f/2 yielded cells richer in 20:4n‐6 (arachidonic acid, ARA: 2.08% vs. 1.38%) and 22:6n‐3 (docosahexaenoic acid, DHA: 6.86% vs. 3.80%). Our results provide evidence that different nitrogen sources may cause variations in the biochemical profile of C. muelleri.     

Characterization of Spatial Variability Structure in Three Separate Field Trials on Pesticide Dissipation

Experiments were carried out on three Italian farms to assess the degree of spatial variation of pesticide field concentration during treatment and during dissipation trials. Test pesticides were chloridazon and metamitron (both sugar-beet herbicides) applied as a tank mix. The classical statistical technique and geostatistics were used to summarize and evaluate variable spatial data. The results show that the actual values of pesticide concentration for application rate and initial concentration in all three areas are lower than expected, thus indicating that under field conditions only a part of the pesticide reaches the soil during the distribution. The actual values for both herbicides in all three areas expressed as percentage of expected values ranged from 44·1% to 64·2% for application rate and from 40·5% to 99·5% for initial concentration. The coefficient of variation was similar for both pesticides and ranged from 23·8 to 74·1 for application rate, 24·1 and 58·8 for initial concentration and 11·1 and 110·0 for dissipation half-lives. The high variability in application rate and initial concentration could be ascribed to an uneven herbicide distribution, and in dissipation studies to variation in half-lives for the rate of herbicide loss from soil in different parts of the field. Geostatistic analysis indicated little spatial correlation, probably because the sampling sites were widely spaced on the field. In all cases, the data were not sufficient to estimate the range of influence, probably because of the size of the experimental fields and the sampling strategy. © 1997 SCI.     

Root Uptake and Xylem Translocation of Pesticides from Different Chemical Classes

A pressure-chamber technique was used to study the root uptake and xylem translocation of some fungicides, herbicides and an insecticide from different chemical classes in detopped soybean roots. Physiological parameters such as K⁺ leakage from roots, K⁺ concentrations in the xylem sap, and protein and ATP levels in the root cells were measured so as to evaluate any potential damage of this technique to the root system. HPLC was used to quantify the compounds in the xylem sap. The pressure-chamber technique has proved useful to study the root uptake and translocation of pesticides, does not damage the root system, and allows one to obtain appreciable volumes of xylem sap that can be analysed directly by HPLC, thus avoiding dependence on the availability of radio-labelled compounds. The concentration of each pesticide in the xylem sap showed a steady-state kinetic profile. Non-linear regression analysis was used to calculate the steady-state concentration and the time required to achieve 50% of the steady-state concentration (TSSC₅₀). TSSC₅₀ was well correlated with log K_ow; the more lipophilic the compound the more time was required to reach the steady-state concentration. The efficiency of translocation was assessed by the transpiration stream concentration factor (TSCF) and a non-linear relationship between TSCF and log K_ow was observed. The highest TSCF values were measured for those compounds with log K_ow values around 3, a lipophilicity value similar to that reported earlier in an analogous experiment with detopped soybean plants but slightly higher than that reported in earlier experiments with intact barley plants. Lower TSCF values were obtained with chemicals with log K_ow values below as well as above 3. © 1997 SCI.