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.

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.

Synthesis and homopolymerization kinetics of 7-(methacroyloxy)-2-oxo-heptylphosphonic acid and its copolymerization with methyl methacrylate.

The synthesis of polymerizable 7-(methacroyloxy)-2-oxo-heptylphosphonic acid M1 destined for self-etch adhesives is described. M1 is characterized by H, C and P-NMR spectroscopy. Its homopolymerization and copolymerization reactivity in the solvents methanol and dioxane between 45 and 70°C in the presence of azobisisobutyronitrile (AIBN) are examined.

α-Glucosidase inhibitory effects of polyphenols from Geranium asphodeloides: Inhibition kinetics and mechanistic insights through in vitro and in silico studies.

Some Geranium species have been used to treat diabetes. To evaluate the scientific basis of this ethnopharmacological use, we aimed to isolate potent α-glucosidase inhibitory metabolites of Geranium asphodeloides Burm. through in vitro bioactivity-guided fractionation.

Synthesis of Branched-Chain Sugars with a DHAP-Dependent Aldolase: Ketones are Electrophile Substrates of Rhamnulose-1-phosphate Aldolases.

Dihydroxyacetone phosphate (DHAP)-dependent rhamnulose aldolases display an unprecedented versatility for ketones as electrophile substrates. We selected and characterized a rhamnulose aldolase from Bacteroides thetaiotaomicron (RhuABthet) to provide a proof of concept. DHAP was added as a nucleophile to several α-hydroxylated ketones used as electrophiles.

Potential of Potentilla inclinata and its polyphenolic compounds in α-glucosidase inhibition: Kinetics and interaction mechanism merged with docking simulations.

In the present study we aimed to identify the α-glucosidase enzyme inhibitory potential of Potentilla inclinata Vill. MeOH and n-BuOH extracts which possessed remarkable α-glucosidase enzyme inhibitory effects with IC values of 1.06±0.

Halogenated 1-Hydroxynaphthalene-2-Carboxanilides Affecting Photosynthetic Electron Transport in Photosystem II.

Series of seventeen new multihalogenated 1-hydroxynaphthalene-2-carboxanilides was prepared and characterized. All the compounds were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach ( L.) chloroplasts.

In vivo magnetic resonance approach to trimethyltin induced neurodegeneration in rats.

Trimethyltin (TMT) is commonly used to induce neurodegeneration in mice and rats; however, only scarce data of in vivo magnetic resonance (MR) spectroscopy and imaging characterizing TMT neurotoxicity are available. Our aim was to assess brain metabolite changes and brain atrophy by in vivo MR in the rat model of neurodegeneration induced by TMT. Adult male Wistar rats exposed to TMT (8mg/kg, i.

Phytochemical Content, Antioxidant and Cytotoxic Activities of Sedum spurium.

Sedum L. species are used for their hemostatic, antidiarrheal, antifungal, diuretic and wound healing properties, and there is growing interest in these species because of their usage in folk medicine. DPPH, SO, NO, and ABTS radical scavenging activities and protective effects against H(2)(02) induced cytotoxicity, as well as cytotoxic activities against the Hep-2 cell line of various extracts from Sedum spurium Bieb.

N-Alkoxyphenylhydroxynaphthalenecarboxamides and Their Antimycobacterial Activity.

A series of nineteen N-(alkoxyphenyl)-2-hydroxynaphthalene-1-carboxamides and a series of their nineteen positional isomers N-(alkoxyphenyl)-1-hydroxynaphthalene-2-carboxamides were prepared and characterized. Primary in vitro screening of all the synthesized compounds was performed against Mycobacterium tuberculosis H37Ra, M. kansasii and M.

In Vitro Metabolomic Approach to Hippocampal Neurodegeneration Induced by Trimethyltin.

Search for indicators of neurodegenerative disorders is a hot topic where much research remains to be done. Our aim was to determine proton nuclear magnetic resonance ((1)H-NMR) spectra of brain metabolites in the trimethyltin (TMT) model of neurodegeneration. Male Wistar rats were subjected to TMT or saline and were sacrificed on day 3 or 24 after administration.

Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents.

In this study, a series of twenty-two ring-substituted 8-hydroxyquinoline-2-carboxanilides was prepared and characterized. Primary in vitro screening of the synthesized compounds was performed against Mycobacterium tuberculosis H37Ra, Mycobacterium avium complex and M. avium subsp.

Neuronal marker recovery after Simvastatin treatment in dementia in the rat brain: in vivo magnetic resonance study.

The aim of study was to search for new biomarkers with a magnetic resonance technique to identify the early stages of dementia, induced by D-galactose, and evaluate Simvastatin therapy. Localized proton magnetic resonance spectroscopy measurements showed a significant decrease in the concentration of N-acetylaspartate+N-acetylaspartylglutamate and myo-inositol in the D-galactose group compared to the control group, and, conversely, an increase of N-acetylaspartate+N-acetylaspartylglutamate in the D-galactose/Simvastatin group. Using a saturation transfer experiment, with phosphorus magnetic resonance spectroscopy, we observed a significant elevation of the forward rate constant of the creatine kinase reaction in the brains of the D-galactose group compared to controls, and subsequently, a significant reduction of this reaction in the D-galactose/Simvastatin group.

Changes in metabolome and in enzyme activities during germination of Trichoderma atroviride conidia.

The aim of this work was to study the metabolic changes during germination of Trichoderma atroviride conidia along with selected marker enzyme activities. The increase in proteinogenic amino acid concentrations together with the increase in glutamate dehydrogenase activity suggests a requirement for nitrogen metabolism. Even though the activities of tricarboxylic acid cycle enzymes also increased, detected organic acid pools did not change, which predisposes this pathway to energy production and supply of intermediates for further metabolism.

Isolation of an oleanane-type saponin active from Bellis perennis through antitumor bioassay-guided procedures.

Context: Bellis perennis L. (Asteraceae) (common daisy) is a herbaceous perennial plant known as a traditional wound herb; it has been used for the treatment of bruises, broken bones, and wounds. Bellis perennis has also been used in the treatment of headache, common cold, stomachache, eye diseases, eczema, skin boils, gastritis, diarrhea, bleeding, rheumatism, inflammation, and infections of the upper respiratory tract in traditional medicine.

Structural analysis of an impurity of the drug landiolol.

In a course of development and preparation of landiolol (1a), a known ultra-short-acting β-blocker, process quality control by HPLC and LC-MS analysis consistently showed an impurity peak ranging from 0.05% to 0.15 % and exhibiting a molecular mass m/z 887.

Polyphenol fatty acid esters as serine protease inhibitors: a quantum-chemical QSAR analysis.

We investigated the ability of polyphenol fatty acid esters to inhibit the activity of serine proteases trypsin, thrombin, elastase and urokinase. Potent protease inhibition in micromolar range was displayed by rutin and rutin derivatives esterified with medium and long chain, mono- and polyunsaturated fatty acids (1e-m), followed by phloridzin and esculin esters with medium and long fatty acid chain length (2a-d, 3a-d), while unmodified compounds showed only little or no effect. QSAR study of the compounds tested provided the most significant parameters for individual inhibition activities, i.

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 (1H, 13C, COSY, HSQC and HMBC) spectroscopy and ESI-TOF-MS.

Isolation, structure elucidation and biological activity of angucycline antibiotics from an epiphytic yew streptomycete.

In the course of study of epiphytic microorganisms occurring on the surface of roots of Taxus baccata L. a new strain Streptomyces sp. AC113 was isolated.

Regular moderate exercise reduces advanced glycation and ameliorates early diabetic nephropathy in obese Zucker rats.

Advanced glycation end products (AGEs) play a key role in the pathogenesis of diabetes and its complications, including the diabetic nephropathy. The renoprotective effects of exercise are well known; however, the mechanisms remain elusive. Here we examined whether a regular moderate exercise in obese Zucker rats (OZR), a model of diabetes- and obesity-associated nephropathy, will affect the development of early renal injury in OZR possibly via alteration of AGEs formation.

Enniatins produced by Fusarium dimerum, an endophytic fungal strain.

Cyclohexadepsipetides enniatin B, B1 and G were isolated from the cultivation broth of Fusarium dimerum Penzig, an endophyte of Magnolia x soulangeana. Their production was about 350 mg l(-1) after 96 h of submerged cultivation in Sabouraud maltose medium. Isolated enniatins inhibited growth of selected microorganisms and activity of 12-lipoxygenase with IC50 = 0.

[Interconversion of stereochemically unstable chiral drugs. Part III: Using beta-cyclodextrin as a chiral stationary phase for HPLC separation of diazepam conformers coupled with an off-line NMR experiment].

Chiral beta-cyclodextrin was used to separate diazepam conformers. Several mobile phases of the composition acetonitrile/acetate buffer 200 mmol/l (pH=3.3, 5.

New magnetic resonance spectroscopy biomarker for monitoring neurodegenerative diseases: animal models.

Creatine kinase (CK) plays a central role in energy transfer in cells with high-energy demands, and the enzyme is rather susceptible to oxidative inactivation. The aim of the present study was to investigate whether the rate constant of forward CK reaction (k(for)) is a suitable indicator of alterations in cerebral energy metabolism. We monitored k(for) in the rat brain non-invasively by in vivo phosphorus ((31)P) magnetic resonance spectroscopy (MRS).

Study of Trichoderma viride metabolism under conditions of the restriction of oxidative processes.

Trichoderma viride was capable of growth and conidiation in the presence of high concentrations of the uncoupler 3,3',4',5-tetrachlorosalicylanilide (up to 100 micromol x L(-1) and of the respiration inhibitor mucidin (up to 100 micromol x L(-1) ) in both submerged and surface cultivation. When vegetative mycelia were cultivated on the solid Czapek-Dox medium with yeast autolysate under an anaerobic and CO2-containing atmosphere, the growth was observed only rarely but the microorganism survived as long as 3 months under these conditions. Major products of metabolism of both aerobic and anaerobic submerged mycelia were identified by means of 1H-NMR measurements.