Hexokinase 2 Inhibition and Biological Effects of BNBZ and Its Derivatives: The Influence of the Number and Arrangement of Hydroxyl Groups

Hexokinase 2 (HK2), an enzyme of the sugar kinase family, plays a dual role in glucose metabolism and mediating cancer cell apoptosis, making it an attractive target for cancer therapy. While positive HK2 expression usually promotes cancer cells survival, silencing or inhibiting this enzyme has been found to improve the effectiveness of anti-cancer drugs and even result in cancer cell death. Previously, benitrobenrazide (BNBZ) was characterized as a potent HK2 inhibitor with good anti-cancer activity in mice, but the effect of its trihydroxy moiety (pyrogallol-like) on inhibitory activity and some cellular functions has not been fully understood. Therefore, the main goal of this study was to obtain the parent BNBZ (2a) and its three dihydroxy derivatives 2b–2d and to conduct additional physicochemical and biological investigations. The research hypothesis assumed that the HK2 inhibitory activity of the tested compounds depends on the number and location of hydroxyl groups in their chemical structure. Among many studies, the binding affinity to HK2 was determined and two human liver cancer cell lines, HepG2 and HUH7, were used and exposed to chemicals at various times: 24 h, 48 h and 72 h. The study showed that the modifications to the structures of the new BNBZ derivatives led to significant changes in their activities. It was also found that these compounds tend to aggregate and exhibit toxic effects. They were found to contribute to: (a) DNA damage, (b) increased ROS production, and (c) disruption of cell cycle progression. It was observed that, HepG2, occurred much more sensitive to the tested chemicals than the HUH7 cells; However, regardless of the used cell line it seems that the increase in the expression of HK2 in cancer cells compared to normal cells which have HK2 at a very low level, is a serious obstacle in anti-cancer therapy and efforts to find the effective inhibitors of this enzyme should be intensified.     

Insect Gut Bacteria Promoting the Growth of Tomato Plants (Solanum lycopersicum L.)

Simple SummaryA new sources of plant growth-promoting (PGP) bacteria are needed to increase the agricultural crops without increasing the usage of chemicals. The aim of this study was to test the hypothesis that insect-gut bacteria promote tomato plant growth. The insect gut bacteria were screened for the presence of PGP traits. The plants treated with bacterial consortium showed a significant increase in fruit yield, in both number of fruits (+41%) and weight of fruits (+44%). Our results showed that: (i) D. virgifera gut’s bacteria significantly promote the growth of tomato plants, and (ii) bacteria other than plant-related can be considered as PGP. It must be underlined that even though the insect gut bacteria were proven to stimulate the plant’s growth, their practical usage must be preceded by an examination of their influence on ecological and biological safety.AbstractWe investigated gut bacteria from three insect species for the presence of plant growth properties (PGP). Out of 146 bacterial strains obtained from 20 adult specimens of Scolytidae sp., 50 specimens of Oulema melanopus, and 150 specimens of Diabrotica virgifera, we selected 11 strains displaying the following: PGP, phosphate solubility, production of cellulase, siderophore, lipase, protease, and hydrogen cyanide. The strains were tested for growth promotion ability on tomato (Lycopersicon esculentum) plants. Each strain was tested individually, and all strains were tested together as a bacterial consortium. Tomato fruit yield was compared with the negative control. The plants treated with bacterial consortium showed a significant increase in fruit yield, in both number of fruits (+41%) and weight of fruits (+44%). The second highest yield was obtained for treatment with Serratia liquefaciens Dv032 strain, where the number and weight of yielded fruits increased by 35% and 30%, respectively. All selected 11 strains were obtained from Western Corn Rootworm (WCR), Diabrotica virgifera. The consortium comprised: Ewingella americana, Lactococcus garvieae, L. lactis, Pseudomonas putida, Serratia liquefaciens, and S. plymuthica. To our knowledge, this is the first successful application of D. virgifera gut bacteria for tomato plant growth stimulation that has been described.     

Developing electrochemical measurements in order to assess anti-corrosive coatings more effectively

The aim of this project was to check reproducibility of results obtained using NOCS (no connection to the substrate) arrangement of the electrochemical noise method (ENM). NOCS involves taking measurements from three nominally identical areas on the coated surface. Thus, no electrical connection to substrate is required. In practice the areas are not identical and various arrangements for connection of the three cells were tried to see if the individual areas could be separated out and whether the individual resistances could be computed. Also different ways of calculating the R_n (noise resistance) and R_sn (spectral noise resistance) parameters were attempted to see which one gave the best comparison with the more standard EIS measurements. The maximum entropy method was recognized to be the most useful for comparison with EIS, as well as for graphic evaluation of results. Regarding distinguishing three areas using different connection arrangements, it was possible to identify the situation when one of the three values was different to the other two. However further experiments are needed before it will be possible to confidently assign an R_n value to each individual area.     

The Impact of Linseed Oil Lipids on the Physical Properties of Corn Crisps and the Possibility of Obtaining Crisps Enriched with n‐3 Fatty Acids

Linseed oil, also known as flaxseed oil, is obtained from the dried, ripened seeds of the flax plant (Linum usitatissimum). The oil is obtained by pressing, sometimes followed by solvent extraction supported by a refining process. Linseed oil is an edible oil that is in demand as a nutritional supplement, as a source of α‐linolenic acid an n‐3 fatty acid. The aim of this work was to investigate: (1) the influence of the corn crisp extrusion process on the degradation of fatty acids in linseed oil (LO) and some preparations obtained from the linseed oil such as ethyl ester (EE) and free fatty acids (FFA) added to the corn in order to increase the nutritional value of the crisps, (2) influence of the oil and two fatty preparations obtained from it on the quality of corn crisps, (3) interaction of the lipid fraction with starch. The extrusion process did not degrade the fatty acids significantly. Expansion ratio obtained in the corn crisp extrusion process decreased from 620 % down to 153 %, the size of pores/thickness of the starch–protein walls forming the structure of the extruded product decreased from 10 μm down to 4 μm, the hardness of the crisps increased from 20 to 75 N, and number of lipid–starch complexes increased with rising polarity of the lipid fraction. FFA were complexed mostly by starch (about 90 %), to a lesser degree by EE (about 60 %) and to the least extent by triacylglycerols (about 10 %). The studies performed under industrial conditions using the single screw extruder for the production of corn crisps with the application of standard parameters of the extrusion process indicated that the addition of a mass of 5 % of the various lipids (triacylglycerols of linseed oil, ethyl esters and fatty acids obtained from linseed oil) to corn grits prior to the extrusion process significantly affect the quality of corn crisps.     

Complex modification effect of linseed cake as an agricultural waste filler used in high density polyethylene composites

Linseed cake (LC) is a by-product of agricultural industry which does not have any large-scale industrial applications. The possibilities of its utilization as filler with plasticizing ability for high density polyethylene (HDPE)-based composites have been investigated. Composites containing 5, 10, 20 and 30 wt% of the waste filler have been prepared using a melt mixing method. The influence of the LC on the mechanical and thermomechanical properties of the composites, as well as their water absorption and morphology, have been evaluated by the following methods: static tensile test, impact strength assessment using Dynstat method, hardness measurements, differential scanning calorimetry, dynamic mechanical thermal analysis, scanning electron microscopy observations, measurements of Vicat’s softening temperature and water uptake test. Application of different measuring techniques allows for describing complex modification effects of the composites’ properties changes induced by the presence of lignocellulosic filler with high oil content. The results of the study proved a pronounced influence of LC on high density polyethylene-based composites, especially a plasticizing effect of crude linseed oil contained by the waste filler particles. LC also has been assumed to affect the polymeric matrix crystallization process. It was found that complex modification of polyethylene results from simultaneously occurring different phenomena including: plasticization of the HDPE by linseed oil, improved crystallinity of the semicrystalline matrix, presence of the rigid lignocellulosic particles dispersed in polymer and accumulation of the oil in the interfacial regions.     

Melt fracture and rheology of linear low density polyethylene ‐ calcium carbonate composites

Rheological behavior and melt fracture of linear low‐density polyethylene (LLDPE) calcium carbonate (CaCO₃) composites were investigated. Two types of commercial inorganic fillers were used, unmodified and modified with stearic acid. Rheological capillary studies were conducted to assess the influence of inorganic filler incorporation as well as chemical treatment on the rheological properties and instability sequence of polyethylene‐based composites. Strong suppression of melt flow instabilities was observed for both types of composites. Mooney analysis was applied to examine the influence of mineral filler addition and stearic acid modification on the wall slip. Moreover, chemical treatment of calcium carbonate allows to obtain better dispersion of the inorganic filler in a polymeric matrix. POLYM. ENG. SCI., 57:998–1004, 2017. © 2016 Society of Plastics Engineers     

The Mechanical Properties of the Novel Nanocrystalline Refractory Tantalum Alloys

Protection of Metals and Physical Chemistry of Surfaces - The nanocrystalline tantalum alloys were investigated in terms of mechanical properties. The materials were obtained by powder metallurgy...     

The Peculiar Structure of Acetobacter pasteurianus CIP103108 LPS Core Oligosaccharide

Acetobacter pasteurianus, a member of the Alphaproteobacteria, is an acetic acid-producing bacterium present on sugar-rich substrates such as such as fruits, flowers and vegetables and traditionally used in the production of fermented food. The preferred living habitat associated with acid conditions makes the structure of the bacterial cell wall interesting to study, due to expected uncommon features. We have used a combination of chemical, analytical and NMR spectroscopy approaches to define the complete structure of the core oligosaccharide from A. pasteurianus CIP103108 LPS. Interestingly, the core oligosaccharide displays a high concentration of negatively charged groups, structural features that might contribute to reinforcing the bacterial membrane.     

Vitamin D Compounds PRI-2191 and PRI-2205 Enhance Anastrozole Activity in Human Breast Cancer Models

1,25-Dihydroxycholecalciferol, the hormonally active vitamin D₃ metabolite, is known to exhibit therapeutic effects against breast cancer, mainly by lowering the expression of estrogen receptors and aromatase activity. Previously, the safety of the vitamin D active metabolite (24R)-1,24-dihydroxycholecalciferol (PRI-2191) and 1,25(OH)₂D₃ analog PRI-2205 was tested, and the in vitro activity of these analogs against different cancer cell lines was studied. We determined the effect of the two vitamin D compounds on anastrozole (An) activity against breast cancer based on antiproliferative activity, ELISA, flow cytometry, enzyme inhibition potency, PCR, and xenograft study. Both the vitamin D active metabolite and synthetic analog regulated the growth of not only estrogen receptor-positive cells (T47D and MCF-7, in vitro and in vivo), but also hormone-independent cancer cells such as SKBR-3 (HER-2-positive) and MDA-MB-231 (triple-negative), despite their relatively low VDR expression. Combined with An, PRI-2191 and PRI-2205 significantly inhibited the tumor growth of MCF-7 cells. Potentiation of the antitumor activity in combined treatment of MCF-7 tumor-bearing mice is related to the reduced activity of aromatase by both An (enzyme inhibition) and vitamin D compounds (switched off/decreased aromatase gene expression, decreased expression of other genes related to estrogen signaling) and by regulation of the expression of the estrogen receptor ERα and VDR.