110 results on '"Joanna Stefańska"'
Search Results
2. The Importance of Substituent Position for Antibacterial Activity in the Group of Thiosemicarbazide Derivatives
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Sara Janowska, Joanna Stefańska, Dmytro Khylyuk, and Monika Wujec
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synthesis of thiosemicarbazide ,structure-activity relationship ,antibacterial activity ,Organic chemistry ,QD241-441 - Abstract
The search for new antibacterial compounds is still a huge challenge for scientists. Each new chemotherapy drug is not 100% effective when introduced into treatment. Bacteria quickly become resistant to known structures. One promising group of new compounds is thiosemicarbazides. In the presented work, we looked for the relationship between structure and antibacterial activity within the group of thiosemicarbazide derivatives. This is a continuation of our previous work. Here, we decided to check to what extent the position of the 3-methoxyphenyl substituent affects potency. We obtained new structures that differ in the positions of the substituent in the thiosemicarbazide skeleton. Based on the obtained results of the biological tests, it can be concluded that the substituent in position 1 of thiosemicarbazide derivatives significantly determines their activity. Generally, among the substituents used, trifluoromethylphenyl turned out to be the most promising. The MIC values for compounds with this substituent are 64 µg/mL towards Staphylococci sp. Using molecular docking, we tried to explain the mechanism behind the antibacterial activity of the tested compounds.
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- 2024
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3. The Effect of Conjugation of Ciprofloxacin and Moxifloxacin with Fatty Acids on Their Antibacterial and Anticancer Activity
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Alicja Chrzanowska, Marta Struga, Piotr Roszkowski, Michał Koliński, Sebastian Kmiecik, Karolina Jałbrzykowska, Anna Zabost, Joanna Stefańska, Ewa Augustynowicz-Kopeć, Małgorzata Wrzosek, and Anna Bielenica
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fluoroquinolone ,conjugation ,fatty acids ,cytotoxicity ,antibacterial activity ,Biology (General) ,QH301-705.5 ,Chemistry ,QD1-999 - Abstract
Novel conjugates (CP) of moxifloxacin (MXF) with fatty acids (1m–16m) were synthesized with good yields utilizing amides chemistry. They exhibit a more pronounced cytotoxic potential than the parent drug. They were the most effective for prostate cancer cells with an IC50 below 5 µM for respective conjugates with sorbic (2m), oleic (4m), 6-heptenoic (10m), linoleic (11m), caprylic (15m), and stearic (16m) acids. All derivatives were evaluated against a panel of standard and clinical bacterial strains, as well as towards mycobacteria. The highest activity towards standard isolates was observed for the acetic acid derivative 14m, followed by conjugates of unsaturated crotonic (1m) and sorbic (2m) acids. The activity of conjugates tested against an expanded panel of clinical coagulase-negative staphylococci showed that the compound (14m) was recognized as a leading structure with an MIC of 0.5 μg/mL denoted for all quinolone-susceptible isolates. In the group of CP derivatives, sorbic (2) and geranic (3) acid amides exhibited the highest bactericidal potential against clinical strains. The M. tuberculosis Spec. 210 strain was the most sensitive to sorbic (2m) conjugate and to conjugates with medium- and long-chain polyunsaturated acids. To establish the mechanism of antibacterial action, selected CP and MXF conjugates were examined in both topoisomerase IV decatenation assay and the DNA gyrase supercoiling assay, followed by suitable molecular docking studies.
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- 2022
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4. Grindelia squarrosa Extract and Grindelic Acid Modulate Pro-inflammatory Functions of Respiratory Epithelium and Human Macrophages
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Barbara Gierlikowska, Agnieszka Filipek, Wojciech Gierlikowski, Dominika Kania, Joanna Stefańska, Urszula Demkow, and Anna K. Kiss
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Grindelia squarrosa ,grindelic acid ,inflammation ,cold syndrome ,respiratory epithelium ,macrophages ,Therapeutics. Pharmacology ,RM1-950 - Abstract
Aim of the study: Both nasal and bronchial epithelial cells have evolved sophisticated mechanisms involved in cellular response to bacterial infection. Recognition of pathogens by TLR receptors activate the NF-κB transcription factor, and lead to production of wide spectrum of cytokines (TNF-α, IL-1β, IL-6 and IL-8). Released by epithelium proinflammatory cytokines intensify migration of macrophages to damaged tissues and modulate their pro-inflammatory functions. Based on traditional use of G. squarrosa aerial parts we hypothesized that successful treatment of cold-related diseases may arise from modulation of the pro-inflammatory functions of respiratory epithelium and human monocytes/macrophages. The biological activity of G. squarrosa extract and grindelic acid were compared with clarithromycin and budesonide used as positive controls.Methods: The expression of surface receptors (TLR-4, IL-10) and expression of adhesive molecules (ICAM-1, VCAM-1, E-selectin) was analyzed with flow cytometry. The macrophage attachment to the epithelial cells was assessed fluorimetrically. The p65 NF-κB concentration and cytokine production was measured spectrophotometrically using enzyme-linked immunosorbent assay. Antibacterial activity was examined by the standard disc-diffusion method and serial dilution method according to CLSI guidelines.Results:G. squarrosa extract and grindelic acid had no antimicrobial effect. However, we noticed significant modulation of pro-inflammatory functions of LPS-stimulated nasal and bronchial epithelium. G. squarrosa extract treatment resulted in decrease of TLR-4 expression and p65 NF-κB concentration and inhibition of cytokines synthesis (IL-8, TNF-α, IL-1β and IL-6) in both cellular models. Additionally, G. squarrosa extract slightly modulated ICAM-1 expression affecting on attachment of macrophages to epithelium. Only G. squarrosa extract was able to stimulate the anti-inflammatory functions of macrophages by inducing TGF-β release and IL-10 receptor surface expression. Grindelic acid, identified as a dominant compound in the plant extract, modulated pro-inflammatory functions of epithelium and macrophages slightly.Conclusion: The obtained results support traditional use of Grindelia squarrosa preparations for a treatment cold-associated diseases symptoms. In our opinion, the observed biological effect of extract may be a consequence of synergistic effect of all compounds present in the extract.
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- 2021
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5. The Cytotoxic Effect of Copper (II) Complexes with Halogenated 1,3-Disubstituted Arylthioureas on Cancer and Bacterial Cells
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Alicja Chrzanowska, Aleksandra Drzewiecka-Antonik, Katarzyna Dobrzyńska, Joanna Stefańska, Piotr Pietrzyk, Marta Struga, and Anna Bielenica
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copper (II) complexes ,thiourea ,cytotoxic activity ,proteome analysis ,antimicrobial activity ,Biology (General) ,QH301-705.5 ,Chemistry ,QD1-999 - Abstract
A series of eight copper (II) complexes with 3-(4-chloro-3-nitrophenyl)thiourea were designed and synthesized. The cytotoxic activity of all compounds was assessed in three human cancer cell lines (SW480, SW620, PC3) and human normal keratinocytes (HaCaT). The complexes 1, 3, 5, 7 and 8 were cytotoxic to the studied tumor cells in the low micromolar range, without affecting the normal cells. The complexes 1, 3, 7 and 8 induced lactate dehydrogenase (LDH) release in all cancer cell lines, but not in the HaCaT cells. They provoked early apoptosis in pathological cells, especially in SW480 and PC3 cells. The ability of compounds 1, 3, 7 and 8 to diminish interleukin-6 (IL-6) concentration in a cell was established. For the first time, the influence of the most promising Cu (II) complexes on intensities of detoxifying and reactive oxygen species (ROS) scavenging the enzymes of tumor cells was studied. The cytotoxic effect of all copper (II) conjugates against standard and hospital bacterial strains was also proved.
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- 2021
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6. Synthesis, Anticancer and Antibacterial Activity of Salinomycin N-Benzyl Amides
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Michał Antoszczak, Ewa Maj, Agnieszka Napiórkowska, Joanna Stefańska, Ewa Augustynowicz-Kopeć, Joanna Wietrzyk, Jan Janczak, Bogumil Brzezinski, and Adam Huczyński
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anticancer activity ,antibacterial activity ,antitubercular activity ,SAR studies ,ionophores ,Organic chemistry ,QD241-441 - Abstract
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.
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- 2014
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7. 1,4-Disubstituted Thiosemicarbazide Derivatives are Potent Inhibitors of Toxoplasma gondii Proliferation
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Katarzyna Dzitko, Agata Paneth, Tomasz Plech, Jakub Pawełczyk, Paweł Stączek, Joanna Stefańska, and Piotr Paneth
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thiosemicarbazide derivatives ,anti-Toxoplasma gondii activity ,antibacterial activity ,bacterial topoisomerases ,toxicity ,docking studies ,DFT calculations ,Organic chemistry ,QD241-441 - Abstract
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.
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- 2014
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8. Antistaphylococcal Activity of Selected Thiourea Derivatives
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Joanna Stefańska, Karolina Stępień, Anna Bielenica, Małgorzata Wrzosek, and Marta Struga
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antistaphylococcal activity ,anti-biofilm activity ,genotoxicity ,thiourea derivatives ,Genetics ,QH426-470 ,Microbiology ,QR1-502 - Abstract
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.
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- 2016
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9. Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies
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Anna Bielenica, Giuseppina Sanna, Silvia Madeddu, Gabriele Giliberti, Joanna Stefańska, Anna E. Kozioł, Oleksandra Savchenko, Paulina Strzyga-Łach, Alicja Chrzanowska, Grażyna Kubiak-Tomaszewska, and Marta Struga
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antimicrobial activity ,biofilm ,cytotoxicity ,thiourea derivatives ,X-ray crystallography ,Organic chemistry ,QD241-441 - Abstract
4-Chloro-3-nitrophenylthioureas 1–30 were synthesized and tested for their antimicrobial and cytotoxic activities. Compounds exhibited high to moderate antistaphylococcal activity against both standard and clinical strains (MIC values 2–64 μg/mL). Among them derivatives with electron-donating alkyl substituents at the phenyl ring were the most promising. Moreover, compounds 1–6 and 8–19 were cytotoxic against MT-4 cells and various other cell lines derived from human hematological tumors (CC50 ≤ 10 μM). The influence of derivatives 11, 13 and 25 on viability, mortality and the growth rate of immortalized human keratinocytes (HaCaT) was observed.
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- 2018
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10. Synthesis and Preliminary Evaluation of the Antimicrobial Activity of Selected 3-Benzofurancarboxylic Acid Derivatives
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Irena Wolska, Joanna Stefańska, Bożena Kuran, Mariola Krawiecka, and Jerzy Kossakowski
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3-benzofurancarboxylic acid ,antimicrobial activity ,antifungal activity ,X-ray diffraction ,Organic chemistry ,QD241-441 - Abstract
Halogen derivatives of selected 3-benzofurancarboxylic acids were prepared using 6-acetyl-5-hydroxy-2-methyl-3-benzofuranocarboxylic acid as starting material. 1H-NMR spectra were obtained for all of the synthesized structures, and for compound VI, an X-ray crystal structure was also obtained. All derivatives were tested for antimicrobial activity against a selection of Gram-positive cocci, Gram-negative rods and yeasts. Three compounds, III, IV, and VI, showed antimicrobial activity against Gram-positive bacteria (MIC 50 to 200 mg/mL). Compounds VI and III exhibited antifungal activity against the Candida strains C. albicans and C. parapsilosis (MIC – 100 mg/mL).
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- 2010
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11. Partnerstwa terytorialne jako sieci organizacyjne. Analiza powiązań w trzech wybranych 'lokalnych grupach działania' w Polsce
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Marek Furmankiewicz and Joanna Stefańska
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partnerstwo terytorialne ,kapitał społeczny ,relacje sieciowe ,Human ecology. Anthropogeography ,GF1-900 ,Social Sciences - Abstract
W artykule analizowany jest charakter powiązań pomiędzy instytucjonalnymi uczestnikami współpracy międzysektorowej w ramach partnerstw terytorialnych (a dokładniej tzw. lokalnych grup działania LEADER) utworzonych na obszarach wiejskich w celu podejmowania wspólnych działań na rzecz rozwoju społeczno-ekonomicznego określonych regionów. W kontekście koncepcji kapitału społecznego, za pomocą podstawowych wskaźników sieciowych, zbadano powiązania w trzech partnerstwach położonych w odrębnych regionach historyczno-kulturowych Polski. Omówiono interakcje pomiędzy uczestnikami współpracy (koordynacja, kooperacja, konflikt, kontrola i konkurencja) oraz przepływy (informacji, środków finansowych, zasobów ludzkich i rzeczowych).
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- 2010
12. Exploring the Role of Relational Practices in Water Governance Using a Game-Based Approach
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Piotr Magnuszewski, Karolina Królikowska, Anna Koch, Michal Pająk, Craig Allen, Victoria Chraibi, Anil Giri, Danielle Haak, Noelle Hart, Michelle Hellman, Donald Pan, Nathan Rossman, Jan Sendzimir, Maggi Sliwinski, Joanna Stefańska, Tharsi Taillieu, Denise Marie Weide, and Ilonka Zlatar
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serious games ,social simulation ,social learning ,relational practices ,river basin management ,water governance ,multi-party collaboration ,stakeholders ,experimental social research ,Hydraulic engineering ,TC1-978 ,Water supply for domestic and industrial purposes ,TD201-500 - Abstract
The growing complexity and interdependence of water management processes requires the involvement of multiple stakeholders in water governance. Multi-party collaboration is increasingly vital at both the strategy development and implementation levels. Multi-party collaboration involves a process of joint decision-making among key stakeholders in a problem domain directed towards the future of that domain. However, the common goal is not present from the beginning; rather, the common goal emerges during the process of collaboration. Unfortunately, when the conflicting interests of different actors are at stake, the large majority of environmental multi-party efforts often do not reliably deliver sustainable improvements to policy and/or practice. One of the reasons for this, which has been long established by many case studies, is that social learning with a focus on relational practices is missing. The purpose of this paper is to present the design and initial results of a pilot study that utilized a game-based approach to explore the effects of relational practices on the effectiveness of water governance. This paper verifies the methods used by addressing the following question: are game mechanisms, protocols for facilitation and observation, the recording of decisions and results, and participant surveys adequate to reliably test hypotheses about behavioral decisions related to water governance? We used the “Lords of the Valley” (LOV) game, which focuses on the local-level management of a hypothetical river valley involving many stakeholders. We used an observation protocol to collect data on the quality of relational practices and compared this data with the quantitative outcomes achieved by participants in the game. In this pilot study, we ran the game three times with different groups of participants, and here we provide the outcomes within the context of verifying and improving the methods.
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- 2018
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13. Thermal analysis, antimicrobial and antioxidant studies of thiosemicarbazone derivatives
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Monika Pitucha, Paweł Ramos, Karolina Wojtunik-Kulesza, Agnieszka Głogowska, Joanna Stefańska, Dorota Kowalczuk, Drózd Monika, and Ewa Augustynowicz-Kopeć
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Physical and Theoretical Chemistry ,Condensed Matter Physics - Abstract
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).
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- 2023
14. Activity of singly and doubly modified derivatives of C20-epi-salinomycin against Staphylococcus strains
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Dominika Czerwonka, Małgorzata Podsiad, Joanna Stefańska, Michał Antoszczak, and Adam Huczyński
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Pharmacology ,Cell Line, Tumor ,Staphylococcus ,Drug Discovery ,Anti-Bacterial Agents ,Pyrans - Abstract
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.
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- 2022
15. Advancements in excited state absorption-based luminescence thermometry
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Joanna Stefańska, Artur Bednarkiewicz, and Lukasz Marciniak
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Materials Chemistry ,General Chemistry - Abstract
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.
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- 2022
16. Painting in the exhibition space, interactions
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Joanna Stefańska
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General Economics, Econometrics and Finance - Abstract
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.
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- 2021
17. Unconventional exhibition spaces as an example of the synergy of architecture and art
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Agata Gawlak, Paulina Kowalczyk, and Joanna Stefańska
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Exhibition ,Painting ,Perception ,media_common.quotation_subject ,Context (language use) ,Narrative ,Art ,Space (commercial competition) ,Architecture ,Function (engineering) ,media_common ,Visual arts - Abstract
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.
- Published
- 2020
18. Cr3+ based nanocrystalline luminescent thermometers operating in a temporal domain
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Joanna Stefańska, Karolina Elzbieciak-Piecka, Lukasz Marciniak, and Daniel Jaque Garcia
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Work (thermodynamics) ,Materials science ,business.industry ,Double exponential function ,General Physics and Astronomy ,02 engineering and technology ,010402 general chemistry ,021001 nanoscience & nanotechnology ,01 natural sciences ,Nanocrystalline material ,Decay curve ,0104 chemical sciences ,Thermal ,Optoelectronics ,Sensitivity (control systems) ,Physical and Theoretical Chemistry ,0210 nano-technology ,business ,Luminescence ,Doped nanocrystals - Abstract
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.
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- 2020
19. Synthesis and evaluation of antibacterial and trypanocidal activity of derivatives of monensin A
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Marta Jędrzejczyk, Natalia Stępczyńska, Greta Klejborowska, Małgorzata Podsiad, Joanna Stefańska, Dietmar Steverding, and Adam Huczyński
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Staphylococcus aureus ,Dose-Response Relationship, Drug ,Molecular Structure ,Trypanosoma brucei brucei ,Organic Chemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Microbial Sensitivity Tests ,Trypanocidal Agents ,Biochemistry ,Anti-Bacterial Agents ,Structure-Activity Relationship ,Parasitic Sensitivity Tests ,Pseudomonas aeruginosa ,Drug Discovery ,Escherichia coli ,Staphylococcus epidermidis ,Molecular Medicine ,Monensin ,Molecular Biology - Abstract
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.
- Published
- 2022
20. Implementing Defects for Ratiometric Luminescence Thermometry
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Karolina Ledwa, Joanna Stefańska, and Lukasz Marciniak
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lanthanide oxide ,Materials science ,Dopant ,terbium ,General Chemical Engineering ,Analytical chemistry ,chemistry.chemical_element ,Phosphor ,Terbium ,Yttrium ,luminescent thermometry ,Emission intensity ,Lutetium ,Nanocrystalline material ,Article ,phosphor ,lcsh:Chemistry ,chemistry ,lcsh:QD1-999 ,General Materials Science ,nanothermometer ,Luminescence ,defects - Abstract
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%/°, C and 2%/°, C for Y2O3:Tb3+ and Lu2O3:Tb3+ nanocrystals, respectively. This study presents the first report on luminescent thermometry using defect emission in inorganic phosphors.
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- 2020
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21. Antibacterial activity of singly and doubly modified salinomycin derivatives
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Adam Huczyński, Karolina Stępień, Michał Sulik, Michał Antoszczak, and Joanna Stefańska
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medicine.drug_class ,Gram-positive bacteria ,Clinical Biochemistry ,Antibiotics ,Pharmaceutical Science ,Context (language use) ,Microbial Sensitivity Tests ,medicine.disease_cause ,01 natural sciences ,Biochemistry ,chemistry.chemical_compound ,Structure-Activity Relationship ,Drug Discovery ,medicine ,Molecular Biology ,Salinomycin ,Pyrans ,biology ,Bacteria ,Molecular Structure ,010405 organic chemistry ,Chemistry ,Mutagenicity Tests ,Organic Chemistry ,Biofilm ,biology.organism_classification ,Combinatorial chemistry ,0104 chemical sciences ,Anti-Bacterial Agents ,Ciprofloxacin ,010404 medicinal & biomolecular chemistry ,Molecular Medicine ,Antibacterial activity ,Genotoxicity ,medicine.drug - Abstract
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.
- Published
- 2020
22. Design and synthesis of novel 1H-tetrazol-5-amine based potent antimicrobial agents: DNA topoisomerase IV and gyrase affinity evaluation supported by molecular docking studies
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Małgorzata Wrzosek, Marta Struga, Michal Kolinski, Sebastian Kmiecik, Anna Bielenica, Daniel Szulczyk, Michał A. Dobrowolski, Wioletta Olejarz, Michał Jóźwiak, Piotr Roszkowski, and Joanna Stefańska
- Subjects
DNA Topoisomerase IV ,Models, Molecular ,0301 basic medicine ,Topoisomerase IV ,Stereochemistry ,Tetrazoles ,Microbial Sensitivity Tests ,01 natural sciences ,DNA gyrase ,Cell Line ,03 medical and health sciences ,chemistry.chemical_compound ,Drug Discovery ,Humans ,Topoisomerase II Inhibitors ,Tetrazole ,Triethylamine ,Amination ,Pharmacology ,Bacteria ,biology ,010405 organic chemistry ,Organic Chemistry ,Bacterial Infections ,General Medicine ,Antimicrobial ,Anti-Bacterial Agents ,0104 chemical sciences ,Molecular Docking Simulation ,030104 developmental biology ,Thiourea ,chemistry ,DNA Gyrase ,Drug Design ,biology.protein ,Sodium azide ,Amine gas treating - Abstract
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).
- Published
- 2018
23. New Type of Nanocrystalline Luminescent Thermometers Based on Ti3+/Ti4+ and Ti4+/Ln3+ (Ln3+ = Nd3+, Eu3+, Dy3+) Luminescence Intensity Ratio
- Author
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Bartłomiej Cichy, Joanna Stefańska, and Lukasz Marciniak
- Subjects
Lanthanide ,Materials science ,Analytical chemistry ,chemistry.chemical_element ,02 engineering and technology ,010402 general chemistry ,021001 nanoscience & nanotechnology ,01 natural sciences ,Nanocrystalline material ,0104 chemical sciences ,Surfaces, Coatings and Films ,Electronic, Optical and Magnetic Materials ,Ion ,General Energy ,Nanocrystal ,chemistry ,Thermometer ,Physical and Theoretical Chemistry ,0210 nano-technology ,Absorption (electromagnetic radiation) ,Luminescence ,Titanium - Abstract
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.
- Published
- 2018
24. Optimization of highly sensitive YAG:Cr3+,Nd3+ nanocrystal-based luminescent thermometer operating in an optical window of biological tissues
- Author
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Joanna Stefańska, Artur Bednarkiewicz, Karolina Trejgis, Lukasz Marciniak, and Wieslaw Strek
- Subjects
education.field_of_study ,Chemistry ,business.industry ,Population ,General Physics and Astronomy ,Phosphor ,Nanotechnology ,02 engineering and technology ,Atmospheric temperature range ,010402 general chemistry ,021001 nanoscience & nanotechnology ,01 natural sciences ,0104 chemical sciences ,Nanocrystal ,Thermometer ,Optoelectronics ,Sensitivity (control systems) ,Physical and Theoretical Chemistry ,0210 nano-technology ,education ,Luminescence ,business ,Excitation - Abstract
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.
- Published
- 2017
25. UHPLC-DAD-MS/MS analysis of extracts from linden flowers (Tiliae flos): Differences in the chemical composition between five Tilia species growing in Europe
- Author
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Anna Pruś, Joanna Stefańska, Karolina A. Pawłowska, Karolina Józefczyk, Maria Ziaja, and Sebastian Granica
- Subjects
0106 biological sciences ,biology ,010405 organic chemistry ,Ms analysis ,Flos ,engineering.material ,biology.organism_classification ,01 natural sciences ,0104 chemical sciences ,Phytochemical ,Tilia ,Botany ,engineering ,Key (lock) ,Medicinal plants ,Agronomy and Crop Science ,Chemical composition ,010606 plant biology & botany ,Lime - Abstract
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.
- Published
- 2020
26. Antistaphylococcal Activity of Selected Thiourea Derivatives
- Author
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Małgorzata Wrzosek, Anna Bielenica, Karolina Stępień, Marta Struga, and Joanna Stefańska
- Subjects
DNA Topoisomerase IV ,Microbiology (medical) ,Staphylococcus aureus ,lcsh:QH426-470 ,Topoisomerase IV ,lcsh:QR1-502 ,010402 general chemistry ,medicine.disease_cause ,01 natural sciences ,Applied Microbiology and Biotechnology ,Microbiology ,lcsh:Microbiology ,chemistry.chemical_compound ,Aniline ,Ciprofloxacin ,Staphylococcus epidermidis ,medicine ,Trifluoromethyl ,biology ,010405 organic chemistry ,genotoxicity ,Thiourea ,General Medicine ,Antimicrobial ,biology.organism_classification ,Anti-Bacterial Agents ,0104 chemical sciences ,lcsh:Genetics ,anti-biofilm activity ,chemistry ,Biofilms ,thiourea derivatives ,biology.protein ,antistaphylococcal activity ,Nuclear chemistry ,medicine.drug - Abstract
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.
- Published
- 2016
27. Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas
- Author
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Grażyna Kubiak-Tomaszewska, Marta Struga, Oleksandra Savchenko, Joanna Stefańska, Silvia Madeddu, Michał Skrzycki, Anna E. Koziol, Tadeusz Lis, Małgorzata Wrzosek, Daniel Szulczyk, Giuseppina Sanna, Gabriele Giliberti, Piotr Tomaszewski, and Sandra Piras
- Subjects
Tryptamine ,DNA Topoisomerase IV ,Staphylococcus aureus ,Indoles ,Topoisomerase IV ,Pharmaceutical Science ,Microbial Sensitivity Tests ,Crystallography, X-Ray ,01 natural sciences ,DNA gyrase ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,chemistry.chemical_compound ,thiourea derivatives of indole ,lcsh:Organic chemistry ,antibacterial activity ,Drug Discovery ,Humans ,Topoisomerase II Inhibitors ,Physical and Theoretical Chemistry ,topoisomerase ,biology ,Molecular Structure ,010405 organic chemistry ,Topoisomerase ,anti-HIV activity ,Organic Chemistry ,Thiourea ,RNA ,0104 chemical sciences ,Anti-Bacterial Agents ,010404 medicinal & biomolecular chemistry ,chemistry ,Biochemistry ,Chemistry (miscellaneous) ,DNA Gyrase ,biology.protein ,antiviral activity ,Molecular Medicine ,DNA supercoil ,Antibacterial activity ,DNA - Abstract
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.
- Published
- 2018
28. One-pot synthesis and antiproliferative activity of novel double-modified derivatives of the polyether ionophore monensin A
- Author
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Joanna Wietrzyk, Greta Klejborowska, Adam Huczyński, Joanna Stefańska, and Ewa Maj
- Subjects
0301 basic medicine ,Staphylococcus aureus ,animal structures ,Stereochemistry ,Ionophore ,Microbial Sensitivity Tests ,medicine.disease_cause ,Biochemistry ,03 medical and health sciences ,chemistry.chemical_compound ,Structure-Activity Relationship ,0302 clinical medicine ,Staphylococcus epidermidis ,Cell Line, Tumor ,Drug Discovery ,medicine ,Humans ,Monensin ,Cell Proliferation ,Pharmacology ,Triphosgene ,biology ,Ionophores ,Organic Chemistry ,Biological activity ,Antimicrobial ,biology.organism_classification ,Amides ,Anti-Bacterial Agents ,030104 developmental biology ,chemistry ,Drug Resistance, Neoplasm ,030220 oncology & carcinogenesis ,Molecular Medicine ,Amine gas treating - Abstract
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.
- Published
- 2018
29. Synthesis, cytotoxicity and antimicrobial activity of thiourea derivatives incorporating 3-(trifluoromethyl)phenyl moiety
- Author
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Małgorzata Wrzosek, Agnieszka Napiórkowska, Marta Struga, Silvia Madeddu, Ewa Augustynowicz-Kopeć, Anna Bielenica, Gabriele Giliberti, Karolina Stępień, Stefano Boi, Giuseppina Sanna, and Joanna Stefańska
- Subjects
DNA Topoisomerase IV ,Aniline Compounds ,Antifungal Agents ,Topoisomerase Inhibitors ,Topoisomerase IV ,Stereochemistry ,Microbial Sensitivity Tests ,Cell Line ,Structure-Activity Relationship ,chemistry.chemical_compound ,Staphylococcus epidermidis ,Drug Discovery ,Humans ,Moiety ,Cytotoxicity ,Cell Proliferation ,Pharmacology ,Trifluoromethyl ,Bacteria ,Dose-Response Relationship, Drug ,Molecular Structure ,biology ,Chemistry ,Organic Chemistry ,Fungi ,Thiourea ,General Medicine ,Antimicrobial ,biology.organism_classification ,Anti-Bacterial Agents ,biology.protein - Abstract
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).
- Published
- 2015
30. Synthesis, antiproliferative and antibacterial evaluation of C-ring modified colchicine analogues
- Author
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Jacek Rutkowski, Katarzyna Popiel, Joanna Stefańska, Adam Huczyński, Franz Bartl, Joanna Wietrzyk, Ewa Maj, and Urszula Majcher
- Subjects
Methicillin-Resistant Staphylococcus aureus ,Stereochemistry ,Antineoplastic Agents ,HL-60 Cells ,Microbial Sensitivity Tests ,medicine.disease_cause ,Mice ,Structure-Activity Relationship ,chemistry.chemical_compound ,Staphylococcus epidermidis ,Cell Line, Tumor ,Drug Discovery ,medicine ,Animals ,Humans ,Colchicine ,Doxorubicin ,Cell Proliferation ,Pharmacology ,Cisplatin ,Mice, Inbred BALB C ,Dose-Response Relationship, Drug ,Molecular Structure ,biology ,Organic Chemistry ,3T3 Cells ,General Medicine ,biology.organism_classification ,Anti-Bacterial Agents ,chemistry ,Staphylococcus aureus ,Amine gas treating ,Drug Screening Assays, Antitumor ,Antibacterial activity ,Derivative (chemistry) ,medicine.drug - Abstract
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.
- Published
- 2015
31. Territorial governance, networks and power: cross‐sectoral partnerships in rural poland
- Author
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Marek Furmankiewicz, Áine Macken-Walsh, and Joanna Stefańska
- Subjects
Economic growth ,Horizontal and vertical ,Political geography ,Corporate governance ,05 social sciences ,Geography, Planning and Development ,0211 other engineering and technologies ,0507 social and economic geography ,021107 urban & regional planning ,Context (language use) ,02 engineering and technology ,Competition (economics) ,Dominance (economics) ,Regional science ,Network governance ,Sociology ,050703 geography ,Social network analysis - Abstract
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.
- Published
- 2014
32. Synthesis, Anticancer and Antibacterial Activity of Salinomycin N-Benzyl Amides
- Author
-
Joanna Wietrzyk, Adam Huczyński, Michał Antoszczak, Ewa Maj, Bogumil Brzezinski, Ewa Augustynowicz-Kopeć, Joanna Stefańska, Jan Janczak, and Agnieszka Napiórkowska
- Subjects
Methicillin-Resistant Staphylococcus aureus ,Spectrometry, Mass, Electrospray Ionization ,Stereochemistry ,Proton Magnetic Resonance Spectroscopy ,Antitubercular Agents ,Pharmaceutical Science ,Antineoplastic Agents ,antitubercular activity ,Microbial Sensitivity Tests ,Crystallography, X-Ray ,medicine.disease_cause ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,Mycobacterium tuberculosis ,Structure-Activity Relationship ,ionophores ,chemistry.chemical_compound ,antibacterial activity ,lcsh:Organic chemistry ,Staphylococcus epidermidis ,Cell Line, Tumor ,Spectroscopy, Fourier Transform Infrared ,Drug Discovery ,medicine ,Humans ,Structure–activity relationship ,Carbon-13 Magnetic Resonance Spectroscopy ,Physical and Theoretical Chemistry ,Salinomycin ,Pyrans ,biology ,Chemistry ,Organic Chemistry ,Hydrogen Bonding ,biology.organism_classification ,Amides ,Combinatorial chemistry ,Anti-Bacterial Agents ,anticancer activity ,SAR studies ,Chemistry (miscellaneous) ,Cell culture ,Staphylococcus aureus ,Molecular Medicine ,Antibacterial activity ,Bacteria - Abstract
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.
- Published
- 2014
33. Phase II Conjugates of Urolithins Isolated from Human Urine and Potential Role of
- Author
-
Jakub P, Piwowarski, Iwona, Stanisławska, Sebastian, Granica, Joanna, Stefańska, and Anna K, Kiss
- Subjects
Adult ,Male ,Biological Products ,Plasma ,Coumarins ,Urinary Tract Infections ,Humans ,Urine ,Hydrolyzable Tannins ,Glucuronidase - Abstract
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[
- Published
- 2017
34. Role of human gut microbiota metabolism in the anti-inflammatory effect of traditionally used ellagitannin-rich plant materials
- Author
-
Anna K. Kiss, Marta Zwierzyńska, Matthias F. Melzig, Patrick Schopohl, Joanna Stefańska, Sebastian Granica, and Jakub P. Piwowarski
- Subjects
Adult ,food.ingredient ,medicine.drug_class ,Anti-Inflammatory Agents ,Gut flora ,Pharmacology ,Anti-inflammatory ,Cell Line ,Feces ,food ,Ellagitannin ,Coumarins ,Drug Discovery ,medicine ,Humans ,Rubus fruticosus ,chemistry.chemical_classification ,Plants, Medicinal ,biology ,Traditional medicine ,Plant Extracts ,Tumor Necrosis Factor-alpha ,Macrophages ,Microbiota ,Middle Aged ,biology.organism_classification ,Hydrolyzable Tannins ,Urolithin ,Rhizome ,Gastrointestinal Tract ,chemistry ,Herb ,Medicine, Traditional ,Rubus - Abstract
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.
- Published
- 2014
35. 1,4-Disubstituted Thiosemicarbazide Derivatives are Potent Inhibitors of Toxoplasma gondii Proliferation
- Author
-
Agata Paneth, Tomasz Plech, Jakub Pawełczyk, Katarzyna Dzitko, Piotr Paneth, Paweł Stączek, and Joanna Stefańska
- Subjects
Staphylococcus aureus ,thiosemicarbazide derivatives ,Stereochemistry ,Antiprotozoal Agents ,Pharmaceutical Science ,DFT calculations ,Inhibitory postsynaptic potential ,Article ,anti-Toxoplasma gondii activity ,Cell Line ,Analytical Chemistry ,lcsh:QD241-441 ,Inhibitory Concentration 50 ,Mice ,Sulfadiazine ,lcsh:Organic chemistry ,Parasitic Sensitivity Tests ,antibacterial activity ,Drug Discovery ,bacterial topoisomerases ,medicine ,Animals ,Topoisomerase II Inhibitors ,Physical and Theoretical Chemistry ,Cytotoxicity ,Molecular Structure ,biology ,Organic Chemistry ,toxicity ,docking studies ,Toxoplasma gondii ,biology.organism_classification ,In vitro ,Anti-Bacterial Agents ,Semicarbazides ,Biochemistry ,Chemistry (miscellaneous) ,Toxicity ,Molecular Medicine ,Female ,Selectivity ,Antibacterial activity ,Toxoplasma ,medicine.drug - Abstract
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.
- Published
- 2014
36. Searching for new derivatives of neocryptolepine: Synthesis, antiproliferative, antimicrobial and antifungal activities
- Author
-
Jessica A. Edward, Arkadiusz Kozubek, Anna Jaromin, Marta Świtalska, Joanna Zagrodzka, Joanna Stefańska, Łukasz Kaczmarek, Joanna Wietrzyk, Piotr Cmoch, Wanda Peczyńska-Czoch, David R. Andes, Robert Zarnowski, Katarzyna Sidoryk, and Wojciech Szczepek
- Subjects
Antifungal Agents ,BALB 3T3 Cells ,Antineoplastic Agents ,Peptide ,Microbial Sensitivity Tests ,Mice ,Structure-Activity Relationship ,chemistry.chemical_compound ,Alkaloids ,Cell Line, Tumor ,Candida albicans ,Drug Discovery ,Animals ,Humans ,Cell Proliferation ,Pharmacology ,chemistry.chemical_classification ,Mice, Inbred BALB C ,Dipeptide ,Dose-Response Relationship, Drug ,Molecular Structure ,biology ,Chemistry ,Organic Chemistry ,Quinoline ,General Medicine ,Fibroblasts ,biology.organism_classification ,Antimicrobial ,In vitro ,Anti-Bacterial Agents ,Amino acid ,Biochemistry ,Biofilms ,Glycine ,MCF-7 Cells ,Quinolines ,Drug Screening Assays, Antitumor - Abstract
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.
- Published
- 2014
37. Synthesis, cytotoxicity and antibacterial activity of new esters of polyether antibiotic – salinomycin
- Author
-
Ewa Maj, Joanna Wietrzyk, Joanna Stefańska, Jan Janczak, Greta Michalska, Katarzyna Popiel, Bogumil Brzezinski, Michał Antoszczak, and Adam Huczyński
- Subjects
Methicillin-Resistant Staphylococcus aureus ,Models, Molecular ,Magnetic Resonance Spectroscopy ,Microbial Sensitivity Tests ,medicine.disease_cause ,Structure-Activity Relationship ,chemistry.chemical_compound ,Staphylococcus epidermidis ,Cell Line, Tumor ,Drug Discovery ,medicine ,Humans ,Doxorubicin ,Cytotoxicity ,Salinomycin ,Pyrans ,Pharmacology ,biology ,Organic Chemistry ,Esters ,General Medicine ,biology.organism_classification ,In vitro ,Anti-Bacterial Agents ,Biochemistry ,chemistry ,Staphylococcus aureus ,Cancer cell ,Drug Screening Assays, Antitumor ,Antibacterial activity ,medicine.drug - Abstract
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.
- Published
- 2014
38. Synthesis, antiproliferative and antibacterial activity of new amides of salinomycin
- Author
-
Joanna Wietrzyk, Bogumil Brzezinski, Adam Huczyński, Ewa Maj, Michał Antoszczak, Joanna Stefańska, and Jan Janczak
- Subjects
Models, Molecular ,BALB 3T3 Cells ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Antineoplastic Agents ,HL-60 Cells ,Microbial Sensitivity Tests ,Biochemistry ,Mice ,Structure-Activity Relationship ,chemistry.chemical_compound ,Staphylococcus epidermidis ,Cell Line, Tumor ,Drug Discovery ,Animals ,Humans ,Structure–activity relationship ,Molecular Biology ,Salinomycin ,Cell Proliferation ,Pyrans ,Bacteria ,Dose-Response Relationship, Drug ,Molecular Structure ,biology ,Cell growth ,Chemistry ,Organic Chemistry ,Fibroblasts ,biology.organism_classification ,Amides ,Anti-Bacterial Agents ,Cell culture ,Cancer cell ,Molecular Medicine ,Drug Screening Assays, Antitumor ,Antibacterial activity - Abstract
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).
- Published
- 2014
39. Differences in Metabolism of Ellagitannins by Human Gut Microbiota ex Vivo Cultures
- Author
-
Joanna Stefańska, Jakub P. Piwowarski, Anna K. Kiss, and Sebastian Granica
- Subjects
0301 basic medicine ,Pharmaceutical Science ,Biology ,Gut flora ,01 natural sciences ,Analytical Chemistry ,03 medical and health sciences ,chemistry.chemical_compound ,Feces ,Ellagitannin ,Drug Discovery ,Humans ,Lythrum ,Pedunculagin ,Nuclear Magnetic Resonance, Biomolecular ,Pharmacology ,chemistry.chemical_classification ,Molecular Structure ,010401 analytical chemistry ,Organic Chemistry ,Casuarictin ,biology.organism_classification ,Hydrolyzable Tannins ,0104 chemical sciences ,Gastrointestinal Microbiome ,030104 developmental biology ,Complementary and alternative medicine ,chemistry ,Biochemistry ,Molecular Medicine ,Casuarinin ,Ex vivo ,Castalagin ,Ellagic acid - Abstract
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.
- Published
- 2016
40. Comparison of antioxidant, anti-inflammatory, antimicrobial activity and chemical composition of aqueous and hydroethanolic extracts of the herb of Tropaeolum majus L
- Author
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Sebastian Granica, Agnieszka Bazylko, E. Osinska, Jakub P. Piwowarski, Anna K. Kiss, Agnieszka Filipek, and Joanna Stefańska
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chemistry.chemical_classification ,Reactive oxygen species ,Antioxidant ,biology ,medicine.drug_class ,Benzyl isothiocyanate ,medicine.medical_treatment ,Quinic acid ,Nasturtium ,biology.organism_classification ,Antimicrobial ,Anti-inflammatory ,Tropaeolum majus ,chemistry.chemical_compound ,chemistry ,Biochemistry ,medicine ,Food science ,Agronomy and Crop Science - Abstract
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.
- Published
- 2013
41. Synthesis and Antibacterial Activity of Some New Derivatives of Thiosemicarbazide and 1,2,4-Triazole
- Author
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Joanna Stefańska, Monika Wujec, Edyta Kuśmierz, Agata Siwek, and Anna Pachuta-Stec
- Subjects
Inorganic Chemistry ,chemistry.chemical_compound ,Cyclohexylacetic acid ,biology ,Chemistry ,Organic Chemistry ,Organic chemistry ,1,2,4-Triazole ,Phenylacetic acid ,biology.organism_classification ,Antibacterial activity ,Biochemistry ,Bacteria - Abstract
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.]
- Published
- 2013
42. Antibacterial Activity and Structure-Activity Relationship Studies of 4- aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides
- Author
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Monika Wujec, Urszula Kosikowska, Katarzyna Dzitko, Joanna Stefańska, Agata Siwek, Anna Malm, and Edyta Kusmierz
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chemistry.chemical_classification ,chemistry.chemical_compound ,chemistry ,Aryl ,Drug Discovery ,Pharmaceutical Science ,Molecular Medicine ,Structure–activity relationship ,Antibacterial activity ,Medicinal chemistry ,Alkyl - Published
- 2013
43. Extracts fromEpilobiumsp. Herbs, Their Components and Gut Microbiota Metabolites ofEpilobiumEllagitannins, Urolithins, Inhibit Hormone-Dependent Prostate Cancer Cells-(LNCaP) Proliferation and PSA Secretion
- Author
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Joanna Stefańska, Anna K. Kiss, Sebastian Granica, Jakub P. Piwowarski, Magdalena Stolarczyk, and Marek Naruszewicz
- Subjects
Pharmacology ,Arginase ,biology ,Biochemistry ,Cell growth ,Epilobium ,LNCaP ,Secretion ,Epilobium hirsutum ,biology.organism_classification ,IC50 ,Epilobium parviflorum - Abstract
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.
- Published
- 2013
44. Spectroscopic, semiempirical studies and antibacterial activity of new urethane derivatives of natural polyether antibiotic – Monensin A
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Mieszko Piśmienny, Adam Huczyński, Bogumil Brzezinski, and Joanna Stefańska
- Subjects
inorganic chemicals ,Hydrogen bond ,Stereochemistry ,Organic Chemistry ,Monensin ,Carbon-13 NMR ,medicine.disease_cause ,Analytical Chemistry ,Inorganic Chemistry ,chemistry.chemical_compound ,chemistry ,Staphylococcus aureus ,Intramolecular force ,medicine ,Moiety ,Antibacterial activity ,Staphylococcus ,Spectroscopy - Abstract
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).
- Published
- 2013
45. Search for Molecular Basis of Antifungal Activity of Thiosemicarbazide Derivatives: A Combined in vitro Antifungal and Enzymatic Studies with in Silico Docking
- Author
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Agata Siwek, Joanna Stefańska, Aleksandra Strzelczyk, and Pawel Staczek
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In silico docking ,Antifungal ,chemistry.chemical_classification ,Enzyme ,Biochemistry ,chemistry ,medicine.drug_class ,Drug Discovery ,medicine ,Pharmaceutical Science ,Molecular Medicine ,In vitro - Published
- 2013
46. X-ray crystallographic, FT-IR and NMR studies as well as anticancer and antibacterial activity of the salt formed between ionophore antibiotic Lasalocid acid and amines
- Author
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Franz Bartl, Bogumil Brzezinski, Ewa Maj, Adam Huczyński, Jacek Rutkowski, Joanna Wietrzyk, Joanna Stefańska, Małgorzata Ratajczak-Sitarz, and Andrzej Katrusiak
- Subjects
Chloroform ,Chemistry ,Stereochemistry ,Butylamine ,Organic Chemistry ,Ionophore ,Protonation ,Antimicrobial ,Medicinal chemistry ,Analytical Chemistry ,Inorganic Chemistry ,chemistry.chemical_compound ,Antibacterial activity ,Cytotoxicity ,Spectroscopy ,Lasalocid - Abstract
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.
- Published
- 2013
47. Hemispheric specialization in domestic dogs (Canis familiaris) for processing different types of acoustic stimuli
- Author
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Adam Kulczyński, Joanna Stefańska, Maciej Trojan, Anna Reinholz-Trojan, and Ewelina Włodarczyk
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Male ,medicine.medical_specialty ,Emotions ,Right cerebral hemisphere ,Stimulus (physiology) ,Audiology ,Lateralization of brain function ,Behavioral Neuroscience ,Dogs ,Orientation ,medicine ,Animals ,Humans ,Brain asymmetry ,Dominance, Cerebral ,Sex Characteristics ,Communication ,biology ,business.industry ,Magnetoencephalography ,General Medicine ,biology.organism_classification ,Animal Communication ,Canis ,Acoustic Stimulation ,Head Movements ,Auditory Perception ,Cats ,Auditory stimuli ,Female ,Animal Science and Zoology ,Functional asymmetry ,Vocalization, Animal ,business ,Psychology - Abstract
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.
- Published
- 2012
48. THIOUREA DERIVATIVES OF 4-AZATRICYCLO[5.2.2.0(2.6)]UNDEC-8-ENE-3,5 DIONE - SYNTHESIS AND BIOLOGICAL ACTIVITY
- Author
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Anna, Bielenica, Joanna, Stefańska, Anna E, Kozioł, Filippo, Iuliano, David, Collu, Guseppina, Sanna, Michał, Jóźwiak, and Marta, Struga
- Subjects
Models, Molecular ,Magnetic Resonance Spectroscopy ,Thiourea ,Humans ,Microbial Sensitivity Tests ,Drug Screening Assays, Antitumor ,Crystallography, X-Ray ,Gram-Positive Bacteria ,Heterocyclic Compounds, 3-Ring ,Anti-Bacterial Agents - Abstract
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.
- Published
- 2016
49. ChemInform Abstract: Synthesis, Dissociation Constants, and Antimicrobial Activity of Novel 2,3-Disubstituted-1,3-thiazolidin-4-one Derivatives
- Author
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Lukasz Popiolek, Anna Malm, Irena Musik, Małgorzata Kiełczykowska, Monika Wujec, Anna Biernasiuk, and Joanna Stefańska
- Subjects
Dissociation constant ,Chemistry ,General Medicine ,Antimicrobial ,Combinatorial chemistry - Published
- 2016
50. Disubstituted thiourea derivatives and their activity on CNS: Synthesis and biological evaluation
- Author
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Bernardetta Busonera, Anna E. Koziol, Gabriele Giliberti, Daniel Szulczyk, Joanna Stefańska, Ewa Kędzierska, Giuseppina Sanna, Sylwia Fidecka, Marta Struga, Barbara Miroslaw, and Paolo La Colla
- Subjects
Central Nervous System ,Male ,Anti-HIV Agents ,Stereochemistry ,Chemistry Techniques, Synthetic ,Motor Activity ,Mice ,chemistry.chemical_compound ,Anti-Infective Agents ,Cell Line, Tumor ,Drug Discovery ,Animals ,Humans ,Endogenous opioid ,Pharmacology ,Bacteria ,Behavior, Animal ,Chemistry ,Aryl ,Organic Chemistry ,Fungi ,Thiourea ,Biological activity ,General Medicine ,Carbon-13 NMR ,Drug Design ,Isothiocyanate ,Proton NMR ,Antibacterial activity - Abstract
A series of new thiourea derivatives of 1,2,4-triazole have been synthesized. The difference in structures of obtained compounds are directly connected with the kind of isothiocyanate (aryl/alkyl). The 1H NMR, 13C NMR, MS methods were used to confirm structures of obtained thiourea derivatives. The molecular structure of (1, 17) was determined by an X-ray analysis. Two of the new compounds (8 and 14) were tested for their pharmacological activity on animal central nervous system (CNS) in behavioural animal tests. The results presented in this work indicate the possible involvement of the serotonergic system in the activity of 8 and 14. In the case of 14 is also a possible link between its activity and the endogenous opioid system. All obtained compounds were tested for antibacterial activity against Gram-positive cocci, Gram-negative rods and antifungal activity. Compounds (1, 2, 5, 7, 9) showed significant inhibition against Gram-positive cocci. Microbiological evaluation was carried out over 20 standard strains and 30 hospital strains. Selected compounds (1–13) were examined for cytotoxicity, antitumor, and anti-HIV activity.
- Published
- 2012
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