Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action

A series of 116 small-molecule 1-hydroxynaphthalene-2-carboxanilides was designed based on the fragment-based approach and was synthesized according to the microwave-assisted protocol. The biological activity of all of the compounds was tested on human colon carcinoma cell lines including a deleted TP53 tumor suppressor gene. The mechanism of activity was studied according to the p53 status in the cell. Several compounds revealed a good to excellent activity that was similar to or better than the standard anticancer drugs. Some of these appeared to be more active against the p53 null cells than their wild-type counterparts. Intercalating the properties of these compounds could be responsible for their mechanism of action

NMR spektroskopia v kvapalnej faze Nove metody a aplikacie pri studiu organickych molekul a biologickych systemov

Available from Slovak Centre of Scientific and Technical Information, under shelf-number: A582781 / Slovenska Technicka Univerzita v BratislaveSIGLESKSlovak Republi

Humic acids characterization by EDXS and 13C NMR spectroscopy

Determination of humic acids spectral characteristics performed fast and convenient method for their quality evaluation. Humic acids (HA) were isolated from five different soil types (Luvi-haplic Chernozem, Haplic Luvisol, Haplic Cambisol, Leptic Cambisol and Eutric Cambisol) and from compost. Basic soil characteristics were determined by commonly used methods. Fractional compositon of humus showed that humic acids content was decreasing in order: compost > Luvi-haplic Chernozem > Haplic Luvisol > Eutric Cambisol > Haplic Cambisol > Leptic Cambisol. Isolated humic acids preparations were characterized comparatively by chemical and spectroscopic methods. Elemental analysis showed the highest carbon content in Luvi-haplic Chernozem HA. The lowest carbon amount was in Eutric Cambisol. Energy–dispersive X-ray spectroscopy detected elements in situ in HA molecule. All samples contained Fe, Cu, Zn, Ti, Ca, K, S, P, Si and Br. Practically no differences in elements content between soil humic substances and compost were detected. The amount of aromatic carbon was higher in Luvi-haplic Chernozem to compare with other samples. Humic acids isolated from Cambisols, on the basis 13C NMR spectroscopic data, showed that all samples contained less aromatic carbon and significantly more aliphatic carbon

A New Acylated Neohesperidoside from Geranium purpureum

A new acylated neohesperoside derivative, 1-octyl-4'-isovaleroyl-neohesperoside (1), was isolated from Geranium purpureum Vill. (Geraniaceae) together with the known compounds quercetin-3-rutinoside and gallic acid. The identification of the isolated compounds was carried out by spectroscopic analysis including 1D- and 2D- NMR (H-1, C-13, COSY, HSQC and HMBC) spectroscopy and ESI-TOF-MS

Effects of creatine and vitamin E on muscle energetic metabolism, antioxidant stability and meat quality of pigs

The effects of supplementing the diet of pigs with creatine monohydrate (CMH) and vitamin E on blood plasma creatine concentration, vitamin E level in muscle, muscle energy metabolism, antioxidant capacity and meat (musculus longissimus dorsi) quality of pigs (DNA tested and negative on malignant hyperthermia) were investigated. Two treatments were used: supplementation with CMH alone (2 g.kg−1 of feed, 10 days before slaughter); and supplementation with both vitamin E (500 mg α-tocopherol.kg−1 of feed for minimum of 30 days) and CMH (2 g.kg−1 of feed, 10 days before slaughter). Pigs supplemented with CMH alone showed elevated plasma creatine concentration (P ≤ 0.05). Phosphorus nuclear magnetic resonance (31P NMR) measurements on post mortem (15 min.) muscle samples showed the highest phosphocreatine levels and ratio PCr/Pi (P ≤ 0.05) in CMH supplemented pigs alone and in combination with vitamin E. Dietary supplementation with vitamin E significantly (P ≤ 0.05) increased the concentration of α-tocopherol in meat. Supplementation with CMH alone or in combination with vitamin E resulted in higher (P = 0.07) a values of loin chops at 5 days of storage. Antioxidative capacity (measured as MDA production after incubation of longissimus muscle homogenates with Fe2+/ascorbate) was substantially improved by vitamin E and somewhat by CMH supplementation

Interactions between Carbon and Nitrogen Metabolism in Fibrobacter succinogenes S85: a (1)H and (13)C Nuclear Magnetic Resonance and Enzymatic Study

The effect of the presence of ammonia on [1-(13)C]glucose metabolism in the rumen fibrolytic bacterium Fibrobacter succinogenes S85 was studied by (13)C and (1)H nuclear magnetic resonance (NMR). Ammonia halved the level of glycogen storage and increased the rate of glucose conversion into acetate and succinate 2.2-fold and 1.4-fold, respectively, reducing the succinate-to-acetate ratio. The (13)C enrichment of succinate and acetate was precisely quantified by (13)C-filtered spin-echo difference (1)H-NMR spectroscopy. The presence of ammonia did not modify the (13)C enrichment of succinate C-2 (without ammonia, 20.8%, and with ammonia, 21.6%), indicating that the isotopic dilution of metabolites due to utilization of endogenous glycogen was not affected. In contrast, the presence of ammonia markedly decreased the (13)C enrichment of acetate C-2 (from 40 to 31%), reflecting enhanced reversal of the succinate synthesis pathway. The reversal of glycolysis was unaffected by the presence of ammonia as shown by (13)C-NMR analysis. Study of cell extracts showed that the main pathways of ammonia assimilation in F. succinogenes were glutamate dehydrogenase and alanine dehydrogenase. Glutamine synthetase activity was not detected. Glutamate dehydrogenase was active with both NAD and NADP as cofactors and was not repressed under ammonia limitation in the culture. Glutamate-pyruvate and glutamate-oxaloacetate transaminase activities were evidenced by spectrophotometry and (1)H NMR. When cells were incubated in vivo with [1-(13)C]glucose, only (13)C-labeled aspartate, glutamate, alanine, and valine were detected. Their labelings were consistent with the proposed amino acid synthesis pathway and with the reversal of the succinate synthesis pathway

Chemical and Phytocoenological Characteristics of Two Different Slovak Peatlands

This paper presents the results of pedological and phytocoenological research focused on the detailed research of chemical parameters (pH, organic carbon, and nutrients), risk elements (As-metalloid, Cd, Co, Cr, Cu, Ni, Pb, and Zn), and species composition of the vegetation of two different peatlands on the territory of Slovakia—Belianske Lúky (a fen) and Rudné (a bog). Sampling points were selected to characterize the profile of the organosol within the peatland, the soil profile between the peatland and the agricultural land, and the soil profile of the outlying agricultural land, which is used as permanent grassland. Based on phytocoenological records, a semi-quantitative analysis of taxa in accordance with the Braun–Blanquet scale was performed. The study revealed that the thickness of the peat horizon of the fen in comparison with the bog is very low. In terms of the quality of organic matter, the monitored peatlands are dominated by fresh plant residues such as cellulose and lignin. Differences between individual types of peatlands were also found in the soil reaction and the supply of nitrogen to the organic matter of peat. The values of the soil exchange reaction were neutral on the fen, as well as slightly alkaline but extremely low on the bog. A significantly higher nitrogen supply was found in the organic matter of the fen in contrast to the bog. At the same time, extremely low content of accessible P and an above-limit content of As in the surface horizons were also found on the fen. From the phytocoenological point of view, 22 plant species were identified on the fen, while only five species were identified on the bog, which also affected the higher diversity (H’) and equitability (e). The results of the statistical testing confirmed the diversity of the studied peatlands and the different impact of environmental variables on plant diversity

Tulips: A Renewable Source of Monomer for Superabsorbent Hydrogels

A new class of superabsorbent hydrogels was synthesized by copolymerization of acrylamide with sodium 4-hydroxy-methylenebutaimate (SHMB). SHMB is obtained by saponification of a-methylene-y-butyrolactone (MBL) which is a renewable monomer from tulips. Radical polymerization of SHMB was studied for the first tin*. The extent of side products through the ring closure depended on the pH used during the polymerization. Reactivity ratios for copolymerization of SHMB with acrylamide were estimated. Prepared hydrogels with various composition were investigated for their swelling, mechanical and thermal properties, and morphology as well as cytotoxicity. The achieved degree of swelling of the hydrogels was up to 82 000% and significantly exceeds the capacity of classical superabsorbent hydrogels made of acrylamide and salts of acrylic acid. The degree of swelling as well as mechanical and thermal properties of the hydrogels could be tuned by SHMB content.European Regional Development Fund through project POLYFRIEND [HUSK 1101/1.2.1/0209]; VEGA grant agency [2/0167/14]; Ministry of Education, Youth and Sports of the Czech Republic-Program NPU I [LO1504