α,β-unsaturated 4-oxo acids in heterocyclic synthesis

3-(1,1-Dioxadibenzothien-4-oyl)acrylic acid (1) was condensed with compounds containing active methylene groups under Michael reaction conditions to furnish the Michael adducts (lactones,2a–c, lactams,3a–c, ketones4a, b). The behavior of these adducts toward the action of hydrazine hydrate were investigated. The compounds were tested for their biological properties. 1st part of this series:Egypt. J. Chem. 42, 309 (1999).     

The production of soluble pyrroloquinoline quinone glucose dehydrogenase by Klebsiella pneumoniae, the alternative host of PQQ enzymes

Klebsiella pneumoniae, which produces PQQ and is available for use with a conventional expression vector system, was selected as the host strain for soluble PQQ glucose dehydrogenase (PQQGDH-B) production. The recombinant K. pneumoniaeexpressed PQQGDH-B in its holo-form at about 18000 U l^–1, equal to that achieved in recombinant Escherichia coli. The signal sequence of recombinant PQQGDH-B produced by K. pneumoniaewas correctly processed. K. pneumoniaecan become an alternative host microorganism not only for PQQGDH-B production but also for recombinant PQQ enzymes production.     

Development of novel liver X receptor modulators based on a 1,2,4-triazole scaffold

Liver?X?Receptor (LXR) agonists have been reported as a potential treatment for atherosclerosis, Alzheimer’s disease and hepatitis C virus (HCV) infection. We have designed and synthesized a series of potent compounds based on a 1,2,4-triazole scaffold as novel LXR modulators. In cell-based cotransfection assays these compounds generally functioned as LXR agonists and we observed compounds with selectivity towards LXRα (7-fold) and LXRβ (7-fold) in terms of potency. Assessment of the effects of selected compounds on LXR target gene expression in HepG2 cells revealed that compounds 6a-b and 8a-b behaved as inverse agonists on FASN expression even though they were agonists in the LXRα and LXRβ cotransfection assays. Interestingly, these compounds had no effect on the expression of SREBP-1c confirming a unique LXR modulator pharmacology. Molecular docking studies and evaluation of ADME properties in-silico show that active compounds possess favorable binding modes and ADME profiles. Thus, these compounds may be useful for in vivo characterization of LXR modulators with unique profiles and determination of their potential clinical utility.     

Stimulation of de novo glutathione synthesis by nitrofurantoin for enhanced resilience of hepatocytes

Cell Biology and Toxicology - Toxicity is not only a function of damage mechanisms, but is also determined by cellular resilience factors. Glutathione has been reported as essential element to...     

The importance of species pool size for community composition

We investigated if an increase in species pool size leads to more pronounced turnover in local communities and assessed if this increase relates to stronger competition for environmental niches or to more random placement of species. We compared compositional turnover of pteridophytes (ferns and lycophytes) at 15 sites in mountain ecosystems on 13 islands in southeast Asia and Melanesia that mainly differed in the size of their species pool. Each site was sampled with 16 plots of 20 × 20 m². Using multiple regression on distance matrices, we investigated the relationship between environmental distance and compositional turnover at different spatial extents within sites with different species pool sizes. Additionally, we tested the hypothesis that the intensity of competition increases with increasing species pool size. This was done by assessing how realized niche overlap and unevenness of communities relate to environmental distance and species pool size. With increasing species pool size, there was an increase in: a) proportional turnover in community composition, b) the importance of environmental distance for explaining turnover in community composition and c) a decrease in environmental niche overlap between species indicating an increasing importance of competition for community composition. Our results support the idea that increasing species pool size increases the competition for available environmental niches, and thereby leads to a tighter connection between environmental factors and community composition.     

Cloning and Heterologous Expression of Hematin-Dependent Catalase Produced by Lactobacillus plantarum CNRZ 1228

Lactobacillus plantarum CNRZ 1228 exhibited heme-dependent catalase activity under environmental conditions similar to those encountered during sausage fermentation. The 1,455-bp catalase gene (katL) was cloned and encoded a protein of 484 amino acids. Expression of katL in a heterologous host showed that katL encodes a functional catalase. PCR screening of selected strains of lactic acid bacteria for katL indicated the presence of similar genes in other strains of lactobacilli.     

Evaluation of target volume and dose accuracy in intrafractional cases of lung cancer based on 4D-CT and 4D-CBCT images using an in-house dynamic thorax phantom

BackgroundThis study aimed to evaluate the target volume and dose accuracy in intrafraction cases using 4-dimensional imaging modalities and an in-house dynamic thorax phantom. Intrafraction motion can create errors in the definition of target volumes, which can significantly affect the accuracy of radiation delivery. Motion management using 4-dimensional modalities is required to reduce the risk.Materials and methodsTwo variations in both breathing amplitude and target size were applied in this study. From these variations, internal target volume (ITVs) contoured in 10 phases of 4D-CT (ITV₁₀), average intensity projection (AIP), and mid-ventilation (Mid-V) images were reconstructed from all 4D-CT datasets as reference images. Free-breathing (FB), augmentation free-breathing (Aug-FB), and static images were also acquired using the 3D-CT protocol for comparisons. In dose evaluations, the 4D-CBCT modality was applied before irradiation to obtain position correction. Then, the dose was evaluated with Gafchromic film EBT3.ResultsThe ITV₁₀, AIP, and Mid-V provide GTVs that match the static GTV. The AIP and Mid-V reference images allowed reductions in ITVs and PTVs without reducing the range of target movement areas compared to FB and Aug-FB images with varying percentages in the range of 29.17% to 48.70%. In the dose evaluation, the largest discrepancies between the measured and planned doses were 10.39% for the FB images and 9.21% for the Aug-FB images.ConclusionThe 4D-CT modality can enable accurate definition of the target volume and reduce the PTV. Furthermore, 4D-CBCT provides localization images during registration to facilitate position correction and accurate dose delivery.     

Prevalence of Escherichia coli in surface waters of Southeast Asian cities

Surface water samples were collected from rivers which fed into large urban areas within Vietnam, Indonesia, Cambodia, and Thailand and were processed to enumerate Escherichia coli. Selected isolates were further characterized using PCR to detect the presence of specific virulence genes. Analyzing the four countries together, the approximate mean cfu/100 ml for E. coli counts in the dry season were log 4.3, while counts in the wet season were log 2.8. Of the 564 E. coli isolates screened for the presence of pathogenic genes, 3.9 % possessed at least one virulence gene. The most common pathogenic types found were Shiga toxin-producing E. coli isolates. These results reinforce the importance of monitoring urban surface waters for fecal contamination, that E. coli in these water environments may serve as opportunistic pathogens, and may help in determining the impact water usage from these rivers have on the public health of urban populations in Southeast Asia.     

Performance of durian shell waste as high capacity biosorbent for Cr(VI) removal from synthetic wastewater

The capability of durian shell waste biomass as a novel and potential biosorbent for Cr(VI) removal from synthetic wastewater was studied. The adsorption study was performed in batch mode at different temperatures and pH. Langmuir and Freundlich isotherm models fit the equilibrium data very well (R² > 0.99). The maximum biosorption capacity of durian shell was 117 mg/g. On modeling its kinetic experimental data, the pseudo-first order prevails over the pseudo-second order model. Thermodynamically, the characteristic of Cr-biosorption process onto durian shell surface was spontaneous, irreversible and endothermic.