Development of Potent Inhibitors of the Mycobacterium tuberculosis Virulence Factor Zmp1 and Evaluation of Their Effect on Mycobacterial Survival inside Macrophages

The enzyme Zmp1 is a zinc‐containing peptidase that plays a critical role in the pathogenicity of Mycobacterium tuberculosis. Herein we describe the identification of a small set of Zmp1 inhibitors based on a novel 8‐hydroxyquinoline‐2‐hydroxamate scaffold. Among the synthesized compounds, N‐(benzyloxy)‐8‐hydroxyquinoline‐2‐carboxamide ( 1 c ) was found to be the most potent Zmp1 inhibitor known to date, and its binding mode was analyzed both by kinetics studies and molecular modeling, identifying critical interactions of 1 c with the zinc ion and residues in the active site. The effect of 1 c on intracellular Mycobacterium survival was assayed in J774 murine macrophages infected with M. tuberculosis H37Rv or M. bovis BCG and human monocyte‐derived macrophages infected with M. tuberculosis H37Rv. Cytotoxicity and genotoxicity were also assessed. Overall, inhibitor 1 c displays interesting in vitro antitubercular properties worthy of further investigation.     

Pitting Corrosion Within Bioreactors for Space Cell-Culture Contaminated by <Emphasis Type="Italic">Paenibacillus glucanolyticus</Emphasis>, a Case Report

Performing cell biology experiments in space imposes the use of hardware that essentially allows fluid exchange in a contained environment. Given the technical and logistical peculiarities, the limited opportunities and the high cost of access to space, a great effort during mission preparation of scientific studies is devoted to preventing loss of the experiment. The European Space Agency (ESA) requires, at the end of the preparation phase, the execution of an Experiment Sequence Test (EST), a dry-run version of the space experiment to check all procedures. At conclusion of the EST of our experiment ‘ENDO’ (ESA ILSRA-2009-1026), we found pitting corrosion of metal parts and biofilm formation within the cell-culture devices. The subsequent chemical (spectral assays), instrumental (OGP SmartScope) and microbiological (MALDI-TOF, 16S rRNA gene sequencing) investigations allowed the identification in contaminated material of Paenibacillus glucanolyticus, a ubiquitous, aerobic, facultative anaerobic, endospore forming, acid-producing, Gram-positive microorganism. A concurrence of P. glucanolyticus contamination and galvanic corrosion determined massive fouling, rust precipitation and damage to cells and cell-culture devices being, to our knowledge, the association between this microbe and corrosion never reported before in literature. As a consequence of the episode a critical procedure of experiment set up, i.e. hardware sterilization, was modified. The ENDO experiment was successfully launched to the International Space Station on September 2nd 2015 and returned to the PI laboratory on September 13th, with all cell culture samples in optimal condition.     

Water Quality Assessment Based on Combined Multi-Criteria Decision-Making Method with Index Method

This work presents combined approach to water quality assessment based on both Water Quality Indices (WQI) and Multi-Criteria Decision-Making (MCDM) methods. Using weights from the official WQI calculation algorithm, the model for MCDM was formed and presented on the case of the Danube River water quality in Serbia. By applying PROMETHEE method, locations of potential environmental risk were determined and ranked according to the quality of water. Using its visual modeling option GAIA, the most dominant variables that affect the quality of water at certain locations were identified as polluting parameters (suspended matter, BOD-5, total N, NH4-N and PO4-P). Concentrations of identified pollutants were compared with limits of both EU and national recommendations so the actual water quality of the river was determined. The results showed that although WQI analysis indicated good and very good water quality, extension with MCDM methods revealed that there is a significant excess in values of PO4-P and E.coli at almost every location on the course of the river, as well as in values of total N and NH4-N. Proposed combined approach could serve to engineers and decision makers involved in water quality management in creating more detailed reports on water quality while facilitating the process of decision-making in the choice of selection of particular locations with critical water quality, where appropriate measures for remediation of pollution should be taken.     

Compatibilized iPP/aPS blends: The effect of the viscosity ratio of the components on the blends morphology

More than 25 PP/PS/SEP blends, where PP is isotactic polypropylene, PS is atactic polystyrene, and SEP is poly(styrene‐block‐ethylene‐co‐propylene), were prepared. The main objective of this study was to investigate the influence of PP/PS viscosity ratio, λ_TM, on the blends' morphology. It was shown that λ_TM strongly influenced not only the overall morphology of the blends, but also the morphology of SEP, which exhibited as many as five different types of structure when blended with PP and/or PS. SEP was found an efficient compatibilizer of PP/PS blends as it decreased the average particle size in all studied systems. An interesting “by‐product” of this work was the discovery of a brand‐new type of polymer morphology, which was called morel structure. The characteristic feature of the morel structure was PS matrix compartmentalized by SEP. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 101: 2236–2249, 2006     

Exploring innovative solutions for aged concrete utilization: treatment of liquid radioactive waste

Clean Technologies and Environmental Policy - In this study, the applicability of waste concrete as a sorbent material for the liquid radioactive waste management was considered. The sample was...     

Optimisation of microwave‐assisted extraction of phenolic compounds from broccoli and its antioxidant activity

The effect of independent variables of microwave‐assisted extraction (MAE), extraction temperature (50–90 °C), microwave power (100–200 W), solvent concentration (methanol/water, 50–90%, v/v) and extraction time (1–27 min) on total phenolics and flavonoids contents as well as antioxidant activity of broccoli extracts was investigated. Response surface methodology was successfully applied for optimisation and the high correlation of the mathematical model indicated that a quadratic polynomial model could be used for optimisation of investigated responses. Considering the maximum amount of extracted total phenolics, total flavonoids and antioxidant activity expressed as ORAC value, the optimal conditions for all three investigated responses were obtained (temperature ?71.11 °C; microwave power ?167.03 W; solvent concentration ?75.95%; and extraction time 16.34 min), which is in agreement with optimal conditions obtained for each investigated responses. The development of simultaneously MAE methods for total phenolics, total flavonoids and antioxidant activity of broccoli extracts might simplify assessment of broccoli as valuables source of antioxidants.