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Synthesis, Antimicrobial Activity, and Tyrosinase Inhibition by Multifunctional 3,4-Dihydroxy-Phenyl Peptidomimetics
Full text linkThe purpose of the present study was to evaluate the synergistic effect of two important pharmacophores, 3,4-dihydroxyphenyl and peptidomimetic moieties, as mushroom tyrosinase inhibitors and antimicrobial agents targeting specific strains of pathogenic bacteria. The 3,4-dihydroxybenzaldehyde (protocatechuic aldehyde) was found to be an effective inhibitor of tyrosinase activity, and due to the fact that it is a safe natural substance with such a scaffolded structure, it is likely that dihydroxyl-substituted phenolic derivatives can exhibit potent tyrosinase inhibitory activity. Series of peptidomimetics with an incorporated 3,4-dihydroxyphenyl scaffold was synthesized and characterized. The inhibitory effects of peptidomimetics on a mushroom tyrosinase were studied. The results showed that among the compounds, five of them showed higher inhibitory activity than the parent 3,4-dihydroxybenzyl aldehyde. In silico docking studies with mushroom tyrosinase (PDB ID 2Y9X) predicted possible binding modes in the enzymatic pocket for these compounds. Furthermore, the antimicrobial activities of peptidomimetics against selected Gram-positive and Gram-negative bacterial strains (E. coli, A. baumannii, P. aeruginosa, E. cloacae, and S. aureus) were investigated. The results showed that all tested peptidomimetics have antimicrobial activities (MIC values from 0.25 to 4.0 μM) comparable with those observed for the commonly used antibiotics (ciprofloxacin, bleomycin, and cloxacillin). Notably, all evaluated compounds demonstrated significant activity against E. coli and S. aureus strains, which are primary sources of infections resulting in numerous fatalities. Additionally, the cytotoxicity of sixteen derivatives was assessed using the MTT assay on BALB/c3T3 mouse fibroblast cell lines. Cytotoxicity analyses indicated that the tested substances have a similar or reduced impact on cell proliferation compared to commonly utilized antibiotics within the range of therapeutic doses. This study presents the potential of peptidomimetics with 3,4-dihydroxyphenyl scaffolds could be beneficial for developing novel tyrosinase inhibitors and new potent food preservatives or cosmetic additives.National Science Center, Poland project OPUS No. 2023/49/B/NZ7/02469;
COST Action EURESTOP, CA21145
Różnorodność przestrzeni podmiejskiej: przykład wiejskiej ulicy na zmieniających się przedmieściach Kijowa
Full text linkThis article explores the heterogeneity of suburban spaces to better understand the characteristics and indicators of diversity within suburbs, emphasising their temporal dimensions and the smallest spatial units exhibiting varied trajectories of change. It aims to discuss the concepts of newness and spatial unevenness in suburban areas and conduct a spatio-temporal analysis of suburban heterogeneity at the level of an individual rural street, using a newly developed methodology for calculating the Index of Uneven Suburban Development (IUSD). The analysis is based on satellite imagery from Google Earth (2005–2022) and fieldwork conducted between 2017 and 2024. A methodology was developed to assess suburban heterogeneity, considering the land functions, spatial, economic, social, and environmental aspects, along with land use types, development patterns, and the accessibility of everyday amenities. Using a rural street in Kyiv’s suburbs as a case study, the article identifies key factors influencing different suburban development trajectories. It highlights differences in landuse patterns between the ‘old’ and ‘new’ sections of the street. Notably, within the ‘new’ section, internal heterogeneity emerges, dividing it into ‘newer wealthier’ and ‘older poorer’ areas, with varying development types and land use. The findings open up new avenues for further discussions on models of suburban space development and future research on urban, suburban, and rural lifestyles, particularly through the lens of the proposed Index of Uneven Suburban Development.Artykuł ten bada heterogeniczność przestrzeni podmiejskich, aby lepiej zrozumieć cechy i wskaźniki różnorodności w obrębie przedmieść, podkreślając ich wymiary czasowe oraz najmniejsze jednostki przestrzenne wykazujące różne trajektorie zmian. Celem jest omówienie pojęć nowości i przestrzennej nierówności na obszarach podmiejskich oraz przeprowadzenie analizy czasowo-przestrzennej heterogeniczności podmiejskiej na poziomie pojedynczej wiejskiej ulicy, przy zastosowaniu nowo opracowanej metodologii obliczania Indeksu Nierównego Rozwoju Podmiejskiego. Analiza opiera się na zdjęciach satelitarnych Google Earth (2005–2022) oraz badaniach terenowych przeprowadzonych w latach 2017–2024. Opracowano metodologię oceny heterogeniczności podmiejskiej, uwzględniającą funkcje terenu, aspekty przestrzenne, ekonomiczne, społeczne i środowiskowe, a także rodzaje użytkowania gruntów, wzory rozwoju oraz dostępność codziennych udogodnień. Na przykładzie wiejskiej ulicy na przedmieściach Kijowa artykuł identyfikuje kluczowe czynniki wpływające na różne trajektorie rozwoju podmiejskiego. Podkreśla różnice we wzorcach użytkowania gruntów między „starymi” i „nowymi” odcinkami ulicy. W szczególności w „nowej” części uwidacznia się wewnętrzna heterogeniczność, dzieląca ją na obszary „nowsze i bogatsze” oraz „starsze i biedniejsze”, charakteryzujące się odmiennymi typami rozwoju i użytkowania gruntów. Wyniki otwierają nowe możliwości dyskusji na temat modeli rozwoju przestrzeni podmiejskiej oraz przyszłych badań nad miejskimi, podmiejskimi i wiejskimi stylami życia, szczególnie w kontekście zaproponowanego Indeksu Nierównego Rozwoju Podmiejskiego
“Overdried, Without Curing? F*Ck, this [Is Supposed to be] Government Licensed Skunk!” Medical Cannabis and the Refracted Publics Within an Online Polish Drug Forum
Full text linkIn this article, we analyze a Polish drug forum as a refracted public by focusing on the intersection of the digital space and illicit substances. To illuminate the reception of the medical cannabis industry in the social worlds of people who use cannabis, we apply qualitative thematic analysis of the content of the major Polish drug forum. The results reveal that there has been a widespread subcultural accommodation of medical cannabis for non-therapeutic use in the form of a backchannel about the quality of cannabis products and ways of obtaining it. We observed the emergence of reflexive narratives, where traditional cultural framing of cannabis as a source of fun and pleasure converged with a narrative of medical purposes and advice counteracting potential harms. The forum holds the emerging cannabis industry “accountable” and accumulates knowledge for the consumers that is otherwise lacking due to the illicit or stigmatized nature of cannabis in Poland. Examining digitally enabled discussions sheds light on the possible social accommodation of cannabis ahead of important societal and legislative transformations.This research is supported by the Polish National Science Centre (NCN) grant 2021/43/B/HS6/00710
VR as an interface between art and technology : enhancing user experience and emotional engagement in a virtual gallery
No full textAbstract In recent years, virtual reality and connected technologies such as augmented and mixed realities, have also enjoyed considerable popularity in architecture and culture. For example, design offices or furniture stores offer their clients the opportunity to walk around a virtual apartment, which is a visualisation of the project for approval and in which the consumer can check how a given arrangement or piece of furniture may look in reality, and not just on paper. However, when it comes to culture, here, we are also dealing with virtual walks, but in this case in art galleries or museums. Visitors can view an exhibition without having to visit a museum in another country, and they can interact with art by touching or viewing objects or paintings from very close, without damaging cultural assets. The chapter introduces to virtual art gallery project aimed to explore capabilities of human perception in VR. It included a comparative analysis of user experience and visual perception using eyetracking. The images, sourced from the BITSCOPE project’s CHIST-ERA IV collection, represent different epoches and art styles. The eyetracking study focused on key areas and gaze plot sequences.The research is a part of project Bitscope (no 2021/03/Y/ST6/00002) supported
by the National Science Centre, Poland, within CHIST-ERA IV from the EU Horizon
2020 Research and Innovation Programme (Grant Agreement no. 857925)
Photochemical Functionalization of 4-Diazoisoquinoline-1,3(2H,4H)-diones and Their 1-Sulfoxide Analogues
No full textIsoquinoline-1,3(2H,4H)-diones have been the subject of numerous studies toward new pharmaceuticals, and therefore novel, mild functionalizations of this scaffold are highly desirable. As diazo compounds are versatile reagents in organic synthesis, 4-diazoisoquinoline-1,3(2H,4H)-diones should give access to a broad range of various derivatives. Indeed, they enable the introduction of fluorinated moieties via photochemical O–H insertion reactions in serviceable yields, typically in under 2 h. Exchanging the 1-carbonyl group with the sulfoxide moiety causes a hypsochromic shift in the absorption of the diazo compounds, and thus, violet light is required for effective O–H and S–H insertion reactions.European Union’s Horizon 2020 Research and Innovation Programme under the Marie Skłodowska–Curie Grant Agreement No. 956324 (MSCA ITN: PhotoReAct
Effects of prior antioxidant supplementation on quality of stored erythrocytes: vitamin C + vitamin E and vitamin C + N-acetylcysteine
No full textBackground The antioxidant status of donors may impact the quality of stored blood and its components. Therefore, oral antioxidant supplementation prior to blood donation could be a promising approach to improve the efficacy of stored erythrocytes. Material and methods Wistar rats (3 months old, n=5/group) were categorized into controls, antioxidant group 1 (vitamin C and vitamin E, VC+VE) and antioxidant group 2 (vitamin C and N-acetylcysteine, VC+NAC). Experimental rats were supplemented for 30 days. Erythrocytes were stored in additive solution (AS-7) for 42 days and analyzed at two-week intervals. Results Hemoglobin increased on days 28 and 42 in both the antioxidant groups. Superoxide dismutase and catalase activities elevated during initial days and, glutathione peroxidase activity towards the end of storage in the antioxidant groups. Protein carbonyls and malondialdehyde levels decreased in the antioxidant groups. Glutathione levels increased on day 42 in VC+VE. Hemolysis was lower in the VC+VE group until day 28 and maintained in the VC+NAC group. Conclusions VC+VE and VC+NAC as supplements protected hemoglobin, blood proteins, and lipids from oxidation and elevated antioxidant defenses. Therefore, prior supplementation augments the antioxidant status and quality of stored blood
“Protecting Americans from Foreign Adversary Controlled Applications Act” – or the Next Installment of the US-China War on TikTok. An Analysis from the Perspective of the Copenhagen School’s Securitisation Theory
No full textThe aim of this article is to examine the circumstances surrounding the Protecting Americans from Foreign Adversary Controlled Applications Act (PAFACA), the controversies it has generated, and the potential threats posed by the TikTok application. Furthermore, it seeks to identify the factors that have facilitated the successful securitisation of TikTok in the United States. In this research, the authors employed a system and legal analysis to situate these regulatory measures within the US legal and political framework. Additionally, monographic and desk research methods were applied. For exploratory purposes, the authors adopted the theory of securitisation, rooted in the constructivist approach. This study represents the first attempt in Polish scholarship to address the US-China competition over ByteDance’s application, filling an existing research gap in this area. Accordingly, the authors have drawn extensively on foreign studies while also referencing Polish-language sources and prior Polish research where relevant. The findings indicate that the securitisation process of TikTok in the US has been successful, showcasing the effectiveness of legislative measures in mitigating digital threats from applications controlled by rival states. This research also provides a valuable foundation for further studies on this topic
Alternatywne formy organizowania się: strategie działania politycznego i troski kobiet w białoruskiej diasporze w Polsce, na Litwie i w Gruzji
No full textIn the aftermath of the 2020 presidential elections in Belarus and the ensuing political crisis, many women were forced into exile. This article explores how Belarusian women continue their engagement in political, socio-cultural, and economic initiatives abroad, often beyond the traditional frameworks of political participation. Drawing on feminist methodology by locating women’s voices as central to inform this research, 10 interviews with women from diasporas in Poland, Lithuania, and Georgia, and ethnographic observation were conducted in 2022. This research includes community support for both Belarusians and Ukrainians, cultural preservation, assistance to political prisoners and migrants, and educational and humanitarian initiatives. The article argues that women’s work in exile not only sustains diasporic life but also constitutes a meaningful form of resistance that challenges dominant notions of visibility, leadership, and political agency. I suggest operationalising non-mainstream political organising through the notion of social reproduction, extending it to the public political domain.Po wyborach prezydenckich na Białorusi w 2020 roku i wynikającym z nich kryzysie politycznym wiele kobiet zostało zmuszonych do emigracji. Artykuł analizuje, w jaki sposób Białorusinki kontynuują swoją działalność polityczną, społeczno-kulturową i ekonomiczną za granicą, często poza tradycyjnymi ramami uczestnictwa politycznego. Opierając się na feministycznej metodologii, poprzez umieszczenie kobiecych głosów w centrum badania, w 2022 roku przeprowadzono 10 wywiadów z kobietami z diaspory w Polsce, na Litwie i w Gruzji oraz obserwację etnograficzną. Tematyka badania obejmuje wsparcie społecznościowe zarówno dla Białorusinów, jak i Ukraińców, działania na rzecz zachowania kultury, pomoc dla więźniów politycznych i migrantów oraz inicjatywy edukacyjne i humanitarne. Artykuł dowodzi, że praca kobiet na emigracji nie tylko podtrzymuje życie diasporyczne, ale stanowi również istotną formę oporu, która kwestionuje dominujące wyobrażenia o widoczności, przywództwie i sprawczości politycznej. Proponuję operacjonalizację niestandardowego organizowania się politycznego poprzez pojęcie reprodukcji społecznej rozszerzonej na publiczną domenę polityczną
Grammatical Devices in Polish Memes About Russia: a Multimodal Analysis
No full textThe main goal of the article is to single out and describe the grammatical devices that generate memes; these are conditioned by both genology and the hyperconnective online communication that contributes to both the formation of the groups of senders-receivers and the shared common ground. The analysis is based on three Russia-themed meme templates (“THAT FEELING WHEN”, “IN SOVIET RUSSIA” and “OUR”). The study inspects the influence of the multimodality of memes on the formation of lexico-grammatical patterns that are adjusted to mediated communication and its brevity, replicability, innovativeness, productivity and cut and driedness.Publication co-financed from the research and research commercialisation fund of the University of Wrocław.
Publication partially funded by the Excellence Initiative – Research University program at the University of Wrocław
Study of tamoxifen derived perfluoroalkylated olefins in breast cancer treatment
No full textEstrogen-responsive breast cancer has been treated with tamoxifen since 1998, yet challenges such as limited selectivity and emerging resistance remain significant hurdles to improving therapeutic outcomes. In recent years, the incorporation of fluorine atoms in the structure of potential drugs has gained importance due to their unique properties. Perfluoroalkyl chains, known for their chemical inertness and ability to target estrogen, offer promising modifications to improve treatment efficacy. In this study, we evaluated the biological activity of 21 perfluoroalkylated tamoxifen derivatives, synthesized under mild conditions with high stereoselectivity. Seven of these compounds exhibited superior cytotoxic and selectivity activity against estrogen receptor-positive breast cancer cells (MCF-7), with IC50 values of 10.68–18.18 nM compared to 29.41 nM for 4-hydroxytamoxifen, which is used in standard therapy. Preliminary mechanism-of-action studies, supported by siRNA knockdown of ESR1 (the estrogen receptor gene), revealed that the compounds act through a similar mechanism to tamoxifen, further confirming their potential as next-generation therapeutic agents for estrogen receptor-positive breast cancer.MICINN (RYC2021-032567-I) funded by MCIN/AEI/10.13039/ 501100011033 and from the European Union «NextGenerationEU»/PRTR»;
Xunta de Galicia (ED481D-2021-020 and ED431F 2023/30);
PI23/01347 and PI20/00497, funded by Spanish National Health Institute Carlos III and co-funded by European Union and FINIBIC (RESISFERRO and ENDOPRO);
InTalent program from UDC-Inditex for the research grant;
Polish National Science Centre (Grants 2019/35/B/ST4/00599);
Universidade da Coruña/CISUG
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