Search

The aim of the presented research was to evaluate the antimicrobial, anti-tuberculosis and antioxidant activity of thiosemicarbazone derivatives. The thermal stability and thermal degradation of nineteen compounds were determined. The results obtained in in vitro tests indicate the potential of selected compounds against Staphylococcus aureus, Staphylococcus epidermidis and Mycobacterium tuberculosis. Some compounds turned out to be active free radical scavengers and at the same time Fe3+ reducing agents. The performed TGA, and c-DTA measurements showed different thermal stable of thiosemicarbazone derivatives. The T2 derivative was the most thermally resistant. On the other hand, the T11 derivative was the least resistant. The performed thermal analysis showed that most of the derivatives underwent two-stage thermal decomposition (13 samples).

Natural polyether ionophore salinomycin (Sal) has been widely used in veterinary medicine as an antibiotic effective in the treatment of coccidian protozoa and Gram-positive bacteria. Moreover, chemical modification of the Sal structure has been found to be a promising strategy to generate semisynthetic analogs with biological activity profiles improved relative to those of the native compound. In this context, we synthesized and thoroughly evaluated the antibacterial potential of a library of C1/C20 singly and doubly modified derivatives of C20-epi-salinomycin, that is, analogs of Sal with inversed stereochemistry at the C20 position. Among the synthesized analog structures, the most promising antibacterial active agents were those obtained via regioselective O-acylation of C20-epi-hydroxyl, particularly esters 7, 9, and 11. Such C20 singly modified compounds showed excellent inhibitory activity against planktonic staphylococci, both standard and clinical strains, and revealed potential in preventing the formation of bacterial biofilms. In combination with their non-genotoxic properties, these Sal derivatives represent attractive candidates for further antimicrobial drug development.

Luminescence thermometry is attracting growing interest from the fundamental research community, which is further stimulated by the needs and challenges of other fields of science and technology.

The article is based on the author's search for the relationship between painting and architecture and experiencing the space in the context of using its potential for painting exhibition. This is a summary of research carried out in 2017- 2019 at the Faculty of Architecture of Poznań University of Technology, entitled "Artwork in architecture". This project aimed to explore the relationship between art and architectural space. Participation in the collective exhibitions, as a part of the first research stage, and the implementation of individual exhibitions in the second stage of the project, have become the basis for author's decisions in this field. The research findings were included in two monographs by a two-person research team, made up of prof. dr hab. Andrzej Maciej Łubowski and dr hab. Joanna Stefańska, titled "SPACES, artwork in architecture" and "RELATIONS, artwork in architecture", PUT Publishing House 2019, 2020. Searching for the best means of recording meaning and emotions connected with the theme of landscape undertaken by the author as well as the thoroughly analysed issue of the functioning of paintings series in the context of the exhibition space, translate into the process of exploration a relationship between artwork and architecture. The exhibition of paintings and selection of proper exhibition space affect an artwork’s reception. The exhibition’s design should exhaust the relationship between contemplation and dialogue in both the painting space and the broader architectural context. It can be stated that the mutual relationship of the artwork and the architectural space surrounding it affects the artwork’s meaning and aesthetics as well as the architecture’s perception.

The article pertains to the relationship between an artwork (painting) and architectural space, as well as the issue of adapting unconventional architectural spaces for an exhibition function in relation to the author's exhibitions presenting the paintings from the same painting series. Different exhibition concepts of each of the exhibitions emphasize the role of a painting in shaping the architectural space and the quality of this space. An artwork becomes a tool that organizes space and influences its quality. At the Faculty of Architecture of Poznań University of Technology, as part of the research project of Professor A.M. Łubowski and J. Stefańska, D.Sc., titled "Artwork in Architecture", there has been research conducted on the correlation of architecture and art. The author was invited to participate in three exhibitions carried out as part of this project. The experiences connected with the project have been described in this article. The problem of using the interiors of buildings whose original purpose was different from exhibiting art , became a part of the author's research carried out in the form of individual and collective exhibitions. Two of them, which took place between 2017 and 2018, showcased paintings from the same series, entitled " I Have Been to Hel(l) and Back. And: Let me Tell you, It Was Wonderful ”, highlighted the importance of the dialogue between architecture and art and created awareness how much this interdependence influences the transformation of the perception of both art and architecture. Appropriate compositional solutions and an appropriate selection of artworks contribute to the complete visual satisfaction of the recipient. Ill-considered combinations cause visual discomfort, which detracts from the potential of both works of art and architectural space. Therefore, it is a need to perform an in-depth analysis of the relationship between the artwork and architectural space, and to avoid conventional, schematic exhibition solutions. The same works placed in various spaces affect the viewer in a different way. The change of the environment influences the change of perception, which creates new interpretative possibilities for the painting’s narrative, while the architectural space gains a wider context of reception through its individualization and increased accessibility. The emotional and intellectual aspect of painting enriches the space with new meanings.

Cr3+ doped nanocrystals were examined as a noncontact temperature sensor in a lifetime-based approach. The impact of both the analysis protocols and host materials on the lifetime-based approach was systematically investigated. Temperature-dependent luminescence decay curves were analyzed according to three different procedures (average lifetime approach, double exponential fit and time-gated ratiometric approach). The advantages and drawbacks of each method are discussed. Additionally, the thermal sensitivities derived from the average lifetime approach and the double exponential fit revealed a strong dependence of the thermal sensitivity of the Cr3+ doped nanocrystals on the crystal field strength. In these cases, it was found that the long metal–oxygen distances in the host materials improve the thermal sensitivity of the system. This work reveals the importance of both host materials and analysis procedures in the lifetime thermal sensitivity of Cr3+ doped nanocrystals and opens up an avenue towards their future optimization.

In luminescence thermometry enabling temperature reading at a distance, an important challenge is to propose new solutions that open measuring and material possibilities. Responding to these needs, in the nanocrystalline phosphors of yttrium oxide Y2O3 and lutetium oxide Lu2O3, temperature-dependent emission of trivalent terbium Tb3+ dopant ions was recorded at the excitation wavelength 266 nm. The signal of intensity decreasing with temperature was monitored in the range corresponding to the 5D4 &rarr, 7F6 emission band. On the other hand, defect emission intensity obtained upon 543 nm excitation increases significantly at elevated temperatures. The opposite thermal monotonicity of these two signals in the same spectral range enabled development of the single band ratiometric luminescent thermometer of as high a relative sensitivity as 4.92%/&deg, C and 2%/&deg, C for Y2O3:Tb3+ and Lu2O3:Tb3+ nanocrystals, respectively. This study presents the first report on luminescent thermometry using defect emission in inorganic phosphors.

The increasing challenge of antibiotic resistance stimulates the search for novel antibacterial agents, especially such that would be effective against multi-drug resistant bacterial strains. Fortunately, natural compounds are excellent sources of potentially new drug leads. Particularly interesting in this context are polyether antibiotic salinomycin (SAL) and its semi-synthetic derivatives, as they exhibit large spectrum of bioactivity. We synthesized and evaluated the antibacterial activity of a series of SAL analogs; four singly (2–3, 15, 17) and two doubly modified (16, 18) derivatives were found to show excellent inhibitory activity not only against planktonic Gram(+) bacterial cells, but also towards select strains of methicillin-resistant staphylococci with the MIC values of 1–4 µg mL−1. Of note, the most promising candidates were more effective in preventing bacterial biofilm formation than unmodified SAL and a commonly used antibiotic – ciprofloxacin. Furthermore, we proved that rational modification of C20 hydroxyl of SAL may reduce genotoxic properties of the obtained analogs. Mechanistically, the structure-activity relationship studies suggested that electroneutral transport mechanism could be beneficial in terms of ensuring high antibacterial activity of SAL derivatives.

The synthesis and biological evaluation of eleven derivatives of the natural polyether ionophore monensin A (MON), modified at the C-26 position, is presented. Eight urethane and three ester derivatives were tested for their antimicrobial activity against different strains of Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli and Pseudomonas aeruginosa. In addition, their antiparasitic activity was also evaluated with bloodstream forms of Trypanosoma brucei. The majority of the modified ionophores were active against a variety of Gram-positive bacterial strains, including methicillin-resistant S. epidermidis, and showed better antibacterial activity than the unmodified MON. The phenyl urethane derivative of MON exhibited the most promising antibacterial activity of all tested compounds, with minimal inhibitory concentration values of 0.25-0.50 μg/ml. In contrast, none of the MON derivatives displayed higher antitrypanosomal activity than the unmodified ionophore.

A total of 14 of 1,5-disubstituted tetrazole derivatives were prepared by reacting appropriate thiourea and sodium azide in the presence of mercury (II) chloride and triethylamine. All compounds were evaluated in vitro for their antimicrobial activity. Derivatives 10 and 11 showed the highest inhibition against Gram-positive and Gram-negative strains (standard and hospital strains). The observed minimal inhibitory concentrations values were in the range of 1–208 μM (0.25–64 μg/ml). Inhibitory activity of 1,5-tetrazole derivatives 10 and 11 against gyrase and topoisomerase IV isolated from S. aureus was studied. Evaluation was supported by molecular docking studies for all synthesized derivatives and reference ciprofloxacin. Moreover, selected tetrazoles (2, 3, 5, 6, 8, 9, 10 and 11) were evaluated for their cytotoxicity. All tested compounds are non-cytotoxic against HaCaT and A549 cells (CC50 ≤ 60 μM).

The spectroscopic properties of YAG:Ti and YAG:Ti,Ln nanocrystalline powders were examined as part of the search for new functional materials devoted to luminescent thermometry. Various temperature-dependent processes occurring in the studied systems were analyzed and the mechanism of absorption and emission of trivalent and tetravalent titanium ions was proposed. The first luminescent thermometer based on the Ti4+/Ti3+ luminescence intensity ratio with maximum sensitivity of 0.71% C–1 is shown. It was shown that the codoping with lanthanide ions enhances the relative sensitivity of YAG:Ti,Ln nanocrystalline luminescent thermometers because of the Ti4+ → Ln3+ energy transfer. The maximal relative sensitivities in the physiological range (2.26% C–1 at 50 °C) were found for YAG:Ti,Nd3+ nanocrystals and the value increases with temperature reaching 3.70% C–1 at 200 °C.

Luminescent and temperature sensitive properties of YAG:Cr3+,Nd3+ nanocrystals were analyzed as a function of temperature, nanoparticle size, and excitation wavelength. Due to numerous temperature-dependent phenomena (e.g. Boltzmann population, thermal quenching, and inter-ion energy transfer) occurring in this phosphor, four different thermometer definitions were evaluated with the target to achieve a high sensitivity and broad temperature sensitivity range. Using a Cr3+ to Nd3+ emission intensity ratio, the highest 3.48% K-1 sensitivity was obtained in the physiological temperature range. However, high sensitivity was compromised by a narrow sensitivity range or vice versa. The knowledge of the excitation and temperature susceptibility mechanisms enabled wise selection of the spectral features found in luminescence spectra for a temperature readout, which enabled the preservation of relatively high temperature sensitivity (>1.2% K-1 max) and extended the temperature sensitivity range from 100 K to 850 K. The size of the nanophosphors had negligible impact on the performance of the studied materials.

Five of thiourea derivatives were prepared using as a starting compound 3-(trifluoromethyl)aniline, 4-chloro-3-nitroaniline, 1,3-thiazol- 2-amine, 2H-1,2,3-triazol-4-amine and commercial isothiocyanates. All compounds were evaluated in vitro for antimicrobial activity. Derivatives 2 and 3 showed the highest inhibition against Gram-positive cocci (standard and hospital strains). The observed MIC values were in the range of 0.5–8 μg/ml. The products effectively inhibited the formation of biofilms of methicillin-resistant and standard strains of Staphylococcus epidermidis. Inhibitory activity of thioureas 2 and 3 against Staphylococcus aureus topoisomerase IV was studied. The examined compounds were nongenotoxic.

Lime flowers are traditionally used as medicinal plants. According to the Pharmacopeia Europaea, only three species of Tilia are admitted as source species. However, so far, no methods enabling the discrimination between these three species and other species of Tilia occurring in Europe have been established. It is also not clear whether the chemical composition of extracts from lime flowers differs between source species. Here, we describe a comprehensive validated UHPLC-DAD-MS/MS method to distinguish the five most important Tilia species in Europe based on phytochemical analyses of extracts prepared from their flowers. Forty-two phenolics were detected in the analyzed extracts and twenty-one of them were quantified using a validated method. A chemometric analysis revealed significant differences between the investigated species. Based on the chemical profile of their extracts, we provide a dichotomous key for the identification of Tiliae flos source species.

A series of 2-(1H-indol-3-yl)ethylthiourea derivatives were prepared by condensation of 2-(1H-indol-3-yl)ethanamine with appropriate aryl/alkylisothiocyanates in anhydrous media. The structures of the newly synthesized compounds were confirmed by spectroscopic analysis and the molecular structures of 8 and 28 were confirmed by X-ray crystallography. All obtained compounds were tested for antimicrobial activity against Gram-positive cocci, Gram-negative rods and for antifungal activity. Microbiological evaluation was carried out over 20 standard strains and 30 hospital strains. Compound 6 showed significant inhibition against Gram-positive cocci and had inhibitory effect on the S. aureus topoisomerase IV decatenation activity and S. aureus DNA gyrase supercoiling activity. Compounds were tested for cytotoxicity and antiviral activity against a large panel of DNA and RNA viruses, including HIV-1 and other several important human pathogens. Interestingly, derivative 8 showed potent activity against HIV-1 wild type and variants bearing clinically relevant mutations. Newly synthesized tryptamine derivatives showed also a wide spectrum activity, proving to be active against positive- and negative-sense RNA viruses.

Monensin A (MON) is a polyether ionophore antibiotic, which shows a wide spectrum of biological activity. New MON derivatives such as double-modified ester-carbonates and double-modified amide-carbonates were obtained by a new and efficient one-pot synthesis with triphosgene as the activating reagent and the respective alcohol or amine. All new derivatives were tested for their antiproliferative activity against two drug-sensitive (MES-SA, LoVo) and two drug-resistant (MES-SA/DX5, LoVo/DX) cancer cell lines, and were also studied for their antimicrobial activity against different Staphylococcus aureus and Staphylococcus epidermidis bacterial strains. For the first time, the activity of MON and its derivatives against MES-SA and MES-SA/DX5 were evaluated.

A total of 31 of thiourea derivatives was prepared reacting 3-(trifluoromethyl)aniline and commercial aliphatic and aromatic isothiocyanates. The yields varied from 35% to 82%. All compounds were evaluated in vitro for antimicrobial activity. Derivatives 3 , 5 , 6 , 9 , 15 , 24 and 27 showed the highest inhibition against Gram-positive cocci (standard and hospital strains). The observed MIC values were in the range of 0.25–16 μg/ml. Inhibitory activity of thioureas 5 and 15 against topoisomerase IV isolated from Staphylococcus aureus was studied. Products 5 and 15 effectively inhibited the formation of biofilms of methicillin-resistant and standard strains of Staphylococcus epidermidis . Moreover, all obtained thioureas were evaluated for cytotoxicity and antiviral activity against a large panel of DNA and RNA viruses. Compounds 5, 6 , 8–12 , 15 resulted cytotoxic against MT-4 cells (CC 50 ≤ 10 μM).

A series of 10 amine derivatives of colchicine have been obtained with high yields by modification at C(10)-OCH3 position of C-ring and characterized by spectroscopic methods. In vitro cytotoxicity has been evaluated against four human tumour cell lines (HL-60, HL-60/vinc, LoVo, LoVo/DX), as well as antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE). From among the compounds tested the most active is colchicine derivative 2h with bis(2-methoxyethyl)amine substituent which is active in nanomolar to submicromolar concentrations and is several times more cytotoxic than cisplatin and doxorubicin. This compound is also effective against the methicillin-resistant Staphylococci strains.

Research on the operation of territorial governance and rural development programmes is dominated by qualitative methodologies, paying little attention heretofore to the characteristics and structures of new horizontal and vertical relationship formations that are the explicit objective of the governance and rural development model. Seeking to address this deficit in the literature, this article adds to a small number of existing contributions that use social network analysis (SNA) to examine the role of inter-organizational networks in shaping geographic functional regions in the context of governance. Rooted in the methodological perspective of SNA, the analysis focuses on relations between local actors participating in three area-based rural partnerships in Poland, which are conceptualized as territorially embedded institutional network clusters. The structure of inter-sectoral relations, understood as interactions (competition, conflict, coordination, cooperation, and control) and flows (information, financial, human, or tangible resources), between the institutional partners of these partnerships is examined. Analysing in detail attributes of network relations, the article identifies structural characteristics of the area-based partnerships, such as manifestations of how diverse local resources are engaged and how dominance by traditional powerful stakeholders can be overcome by network structures. Structural dynamics and transformations that represent expressions and manifestations of how territorially embedded governance networks are expected to operate are important areas of inquiry in political geography. In this context, the particular empirical and theoretical capacity of SNA is illuminated in this article as part of a broader presentation of primary field data on how network governance and rural development is taking shape in Central and Eastern Europe.

In recent years, many xenobiotics derived from natural products have been shown to undergo extensive metabolism by gut microbiota. Ellagitannins, which are high molecular polyphenols, are metabolized to dibenzo[

A series of 12 novel monosubstituted N-benzyl amides of salinomycin (SAL) was synthesized for the first time and characterized by NMR and FT-IR spectroscopic methods. Molecular structures of three salinomycin derivatives in the solid state were determined using single crystal X-ray method. All compounds obtained were screened for their antiproliferative activity against various human cancer cell lines as well as against the most problematic bacteria strains such as methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE), and Mycobacterium tuberculosis. Novel salinomycin derivatives exhibited potent anticancer activity against drug-resistant cell lines. Additionally, two N-benzyl amides of salinomycin revealed interesting antibacterial activity. The most active were N-benzyl amides of SAL substituted at -ortho position and the least anticancer active derivatives were those substituted at the -para position.

Ethnopharmacological relevance Ellagitannin-rich plant materials are widely used in traditional medicine as effective, internally used anti-inflammatory agents. Due to the not well-established bioavailability of ellagitannins, the mechanisms of observed therapeutic effects following oral administration still remain unclear. The aim of the study was to evaluate if selected ellagitannin-rich plant materials could be the source of bioavailable gut microbiota metabolites, i.e. urolithins, together with determination of the anti-inflammatory activity of the metabolites produced on the THP-1 cell line derived macrophages model. Materials and Methods The formation of urolithins was determined by ex vivo incubation of human fecal samples with aqueous extracts from selected plant materials. The anti-inflammatory activity study of metabolites was determined on PMA differentiated, IFN-γ and LPS stimulated, human THP-1 cell line-derived macrophages. Results The formation of urolithin A, B and C by human gut microbiota was established for aqueous extracts from Filipendula ulmaria (L.) Maxim. herb (Ph. Eur.), Geranium pratense L. herb, Geranium robertianum L. herb, Geum urbanum L. root and rhizome, Lythrum salicaria L. herb (Ph. Eur.), Potentilla anserina L. herb, Potentilla erecta (L.) Raeusch rhizome (Ph. Eur.), Quercus robur L. bark (Ph. Eur.), Rubus idaeus L. leaf, Rubus fruticosus L. and pure ellagitannin vescalagin. Significant inhibition of TNF-α production was determined for all urolithins, while for the most potent urolithin A inhibition was observed at nanomolar concentrations (at 0.625 μM 29.2±6.4% of inhibition). Urolithin C was the only compound inhibiting IL-6 production (at 0.625 μM 13.9±2.2% of inhibition). Conclusions The data obtained clearly indicate that in the case of peroral use of the examined ellagitannin-rich plant materials the bioactivity of gut microbiota metabolites, i.e. urolithins, has to be taken under consideration.

A series of 4-arylthiosemicarbazides substituted at the N1 position with a 5-membered heteroaryl ring was synthesized and evaluated in vitro for T. gondii inhibition proliferation and host cell cytotoxicity. At non-toxic concentrations for the host cells all studied compounds displayed excellent anti-parasitic effects when compared to sulfadiazine, indicating a high selectivity of their anti-T. gondii activity. The differences in bioactivity investigated by DFT calculations suggest that the inhibitory activity of 4-aryl-thiosemicarbazides towards T. gondii proliferation is connected with the electronic structure of the molecule. Further, these compounds were tested as potential antibacterial agents. No growth-inhibiting effect on any of the test microorganisms was observed for all the compounds, even at high concentrations.

A series of novel amino acid and dipeptide derivatives of neocryptolepine were synthesized and tested for their antimicrobial, antifungal and antiproliferative activity in vitro against cancer cell lines (KB, A549, MCF-7, LoVo) and normal mice fibroblast cells (BALB/3T3). Biological evaluation revealed that almost all of the new compounds displayed high antiproliferative activity against the tested cells and moderate to potent antibacterial activities. Interestingly, these compounds were active against Candida albicans biofilms at doses significantly lower than those required against free-floating planktonic fungal cells. The most promising compounds are derivatives with glycine and L-proline as a substituent both at 2 and at 9 position of 5H-indolo[2,3-b]quinoline. In general, these new compounds (2a, 3a, 6a and 7a) showed the highest dual action against cancer lines and infectious pathogenic microbes in vitro.

A series of 12 novel ester derivatives of naturally occurring polyether antibiotic - salinomycin were synthesized, characterised by spectroscopic method and evaluated for their in vitro antibacterial activity and cytotoxicity. The new esters were demonstrated to form complexes with monovalent and divalent metal cation of 1:1 stoichiometry in contrast to the salinomycin which forms only complexes with monovalent cations. All the obtained compounds show potent antiproliferative activity against human cancer cell lines and a good selectivity index for cancer versus mammalian cells. Additionally, 3 compounds showed higher antiproliferative activity against the drug-resistant cancer cells and lower toxicity towards normal cells than those of unmodified salinomycin and standard anticancer drugs such as cisplatin and doxorubicin. Some of the synthesized compounds showed good inhibitory activity against Staphylococcus strains and clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE). These studies show that salinomycin esters are interesting scaffolds for the development of novel anticancer and Gram-positive antibacterial agents.

A series of 11 novel amides of salinomycin were synthesized for the first time. All the obtained compounds were found to show potent antiproliferative activity against human cancer cell lines including the drug-resistant cancer cells. Four new salinomycin derivatives revealed good antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus epidermidis (MRSE).

Ellagitannin-rich plant materials are used as popular remedies in the treatment of various inflammatory diseases. Urolithins are gut microbiota metabolites of ellagitannins and are considered responsible for in vivo health effects. Various natural products have been studied that are known sources of urolithins. However, few studies have focused on the metabolism of ellagitannin molecules. The aim of the study was to examine the metabolic fate of select ellagitannins using ex vivo cultures of human gut microbiota. Fifteen monomeric and dimeric ellagitannins, 1-O-galloyl-4,6-(S)-HHDP-β-d-glucose (2), pedunculagin (3), potentillin (4), casuarictin (5), coriariin B (6), vescalagin (7), castalagin (8), stachyurin (9), casuarinin (10), stenophyllinin A (11), stenophyllanin A (12), salicarinin A (13), gemin A (14), agrimoniin (15), and oenothein B (16), and ellagic acid (1) were studied. The formation of the metabolites in ex vivo human microbiota cultures was monitored using UHPLC-DAD-MS/MS. Ellagitannins possessing hexahydroxydiphenoyl moieties were metabolized to 6H-dibenzo[b,d]pyran-6-one derivatives, i.e., urolithins. The observed differences in amounts of produced urolithins indicated that the individual microbiota composition and type of ingested ellagitannins could determine the rate of urolithin production. When the oral ingestion of natural products containing ellagitannins with hexahydroxydiphenoyl groups is considered, the formation of urolithins and their bioactivity should be addressed.

The aim of this study was comparison of antioxidant, anti-inflammatory, and antimicrobial activity, as well as chemical composition of extracts of Tropaeolum majus L. herb. Aqueous and hydroethanolic extracts derived from dried and freeze-dried nasturtium herb, prepared both at room temperature and at 90 °C, were studied. In the studies there were no significant differences between antioxidant activity of the extracts. All extracts showed scavenging activity against all the examined reactive species in a concentration-dependent manner. The strongest scavenging activity they showed against reactive nitrogen species, NO (SC50 4.54 ± 0.26–10.90 ± 1.39 μg/mL) and ONOO − (SC50 2.49 ± 1.50–6.37 ± 1.86 μg/mL). Among reactive oxygen species, they showed strong scavenging activity against H 2 O 2 (SC50 14.90 ± 3.91–38.63 ± 9.28 μg/mL). Scavenging activity against O 2 − was weaker, while against HClO the extracts showed very weak activity, practically at the level of statistical error. Against synthetic radical – DPPH scavenging activity of the tested extracts was negligible. The extracts demonstrated stronger antioxidant activity in ex vivo experiment on human neutrophils. The extracts showed no inhibitory activity on hyaluronidase, but at a concentration of 50 μg/mL they inhibited the activity of COX1 by approximately 60%. Lack of antimicrobial activity of the extracts seems to be associated with a low content of benzyl isothiocyanate. The aqueous extracts were characterized by the presence of esters of quinic acid with cinnamic acids (chlorogenic acids, p-coumaroylquinic acids) and the presence of flavonoids. Meanwhile the hydroethanolic extracts were mainly rich in the above mentioned acid esters.

In a reaction of hydrazides of cyclohexylacetic acid 1 and phenylacetic acid 2 with isothiocyanates, respective thiosemicarbazide derivatives 3–18 were obtained. Further cyclization with 2% NaOH led to the formation of 5-(cyclohexylmethyl/benzyl)-4-substituted-2,4-dihydro-3H-1,2,4-triazole-3-thiones 19–34. Structures of all new products were confirmed by analytical and spectroscopic methods. All compounds were screened for their in vitro activity against some species of bacteria and fungi. [Supplementary materials are available for this article. Go to the publisher's online edition ofPhosphorus, Sulfer, and Silicon and the Related Elements for the following free supplemental files: Additional figures and tables.]

Extracts from Epilobium sp. herbs have been traditionally used in the treatment of prostate-associated ailments. Our studies demonstrated that the extracts from Epilobium angustifolium, Epilobium parviflorum and Epilobium hirsutum herbs are potent prostate cancer cells (LNCaP) proliferation inhibitors with IC50 values around 35 mg/ml. The tested extracts reduced prostate specific antigen (PSA) secretion (from 325.625.3 ng/ml to ~90 ng/ml) and inhibited arginase activity (from 65.21.1 mUnits of urea/mg of protein to ~40 mUnits of urea/mg protein). Selected constituents of extracts (oenothein B, quercetin-3-O-glucuronide, myricetin-3-O-rhamnoside) were proventobeactiveinrelationtoLNCaPcells.However,oenotheinBwasthestrongestinhibitorofcellsproliferation (IC50=7.80.8 mM), PSA secretion (IC50=21.93.2 mM) and arginase activity (IC50=19.22.0 mM). Additionally, ellagitannins from E. hirustum extract were proven to be transformed by human gut microbiota into urolithins. Urolithin C showed the strongest activity in the inhibition of cell proliferation (IC50=35.23.7 mM), PSA secretion (reduced PSA secretion to the level of 100.731.0 ng/ml) and arginase activity (reduced to the level of 27.93.3 mUnits of urea/mg of protein). Results of the work offer an explanation of the activity of Epilobium extractsand supporttheuseof Epilobium preparationsin thetreatment of prostate diseases. Copyright © 2013 John Wiley & Sons, Ltd.

A series of new Monensin A dimers linked by diurethane moiety were synthesised and their molecular structures were studied using ESI-MS, FT-IR, 1 H and 13 C NMR and PM5 methods. The results showed that the compounds form a pseudo-cyclic structure stabilized by three intramolecular hydrogen bonds and the sodium cation was coordinated by five oxygen atoms of polyether skeleton of Monensin moiety. The NMR and FT-IR data of complexes of Monensin urethane sodium salts demonstrated that within the pseudo-cyclic structure the carbonyl oxygen atom of the urethane group did not coordinate the sodium cation. Monensin urethanes were tested in vitro for the activity against Gram-positive and Gram-negative bacteria and fungi as well as against a series of clinical isolates of Staphylococcus : methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive S. aureus (MSSA). The most active compound against MRSA and MSSA was 1,4-phenylene diurethane of Monensin with MIC 10.4–41.4 μmol/L).

Two new complexes of the ionophore antibiotic Lasalocid acid (LAS) with phenylamine (PhA) and butylamine (BuA) were synthesized and their molecular structures were studied using single crystal X-ray diffraction and spectroscopic methods. In the solid state both amines are protonated and all NH 3 + protons are hydrogen bonded to etheric, hydroxyl and carboxylic oxygen atoms of the LAS anion. In chloroform solutions the structure observed in the crystal of LAS–BuA complex is preserved and an equilibrium between the LAS–PhA complex and dissociated Lasalocid acid and phenylamine is observed. In vitro antimicrobial tests of the complexes showed a significant activity towards some strains of Gram-positive bacteria. For the first time Lasalocid acid and its complexes with amines were tested in vitro for cytotoxic activity against human cancer cell lines: A-549 (lung), MCF-7 (breast), HT-29 (colon) and mouse cancer cell line P-388 (leukemia). We found that LAS and its complexes are strong cytotoxic agents towards all tested cell lines. The cytostatic activity of the compounds studied is greater than that of cisplatin, indicating that Lasalocid and its complexes are promising candidates for new anticancer drugs.

A series of halogeno derivatives of thiourea bearing a polycyclic imide core has been efficiently synthesized and evaluated for antimicrobial activity. The structures of the compounds were established by 1H and 13C NMR and MS methods. The molecular structure of 4Clc was determined by an X-ray crystallography. Compounds containing 3-chloro-4-fluorophenyl substituent (3Cl4Fb, 3Cl4Fd) were found to be the most promising against Gram-positive bacteria (MIC values ranged from 8 to 32 pg/mL for standard and 32 - 64 µg/mL for hospital strains). The in vitro cytotoxicity against MT-4 cells of all compounds was evaluated.

Lateralization is considered to be a fundamental feature of vertebrate brains. The aim of the present study was to examine the impact of functional cerebral asymmetry on processing of auditory stimuli in the domestic dog ( Canis familiaris ) during the orientation reaction. The experiment was conducted on 46 dogs (25 females and 21 males). Four types of auditory stimuli were used in the experiment (three meaningful stimuli: cat meowing, dog barking, the “sit” command (“siad” in Polish), and a neutral word (“wir”, meaning “whirl” in Polish). It was predicted that the orientation reaction (turning the head towards the stimuli) would take place only in the case of meaningful sounds. It was also expected that dogs would show consistent lateralization. As predicted, all three meaningful stimuli elicited the orientation reaction. The response of the examined dogs to cat meowing showed significant lateralization with dominant leftwards movement, which hints towards activation of the right cerebral hemisphere and may be related to strong emotions evoked by this stimulus. Contrary to results of previous studies, dogs reacting to dog barking turned their heads leftwards more often, which suggests activation of the right cerebral hemisphere, probably related to the emotional meaning of the stimulus. The “sit” command consistently evoked the orientation reaction but there was no significant lateralization of this movement.