@article{MTMT:35594147, title = {Selenocompounds as Potent Efflux Pump Inhibitors on Gram‐positive Bacteria}, url = {https://m2.mtmt.hu/api/publication/35594147}, author = {Kincses, Annamária and Szemerédi, Nikoletta and Benito‐Lama, Miguel and Dózsai, Dávid and Csonka, Ákos and Domínguez‐Álvarez, Enrique and Spengler, Gabriella}, doi = {10.1002/cmdc.202400691}, journal-iso = {CHEMMEDCHEM}, journal = {CHEMMEDCHEM}, unique-id = {35594147}, issn = {1860-7179}, abstract = {In recent years, selenocompounds have gained increasing attention as potential anticancer and antibacterial agents. Several selenoderivatives have been confirmed to act as MDR efflux pump inhibitors, based on their in vitro results against the bacterial AcrAB‐TolC system and the cancer MDR efflux pump P‐glycoprotein. Efflux pumps can contribute directly or indirectly to the virulence of bacteria, as they can reduce the intracellular concentration of antibacterial substances by expelling them out of the cell. The present work aims to study the antibacterial and efflux pump inhibiting properties of four families of selenoesters, namely aspirin‐selenoesters, phenone‐selenoesters, hydroxy‐selenoesters, and benzyl‐selenoesters. The real‐time ethidium bromide accumulation assay confirmed that these derivatives inhibited the efflux systems of methicillin‐resistant Staphylococcus aureus (MRSA) without exerting any antibacterial effect. The relative expression of efflux pump gene of NorA transporter was also monitored in the presence of the most potent derivatives on reference S. aureus , finding that these derivatives could change the expression of the tested efflux pump gene. Regarding the anti‐biofilm activity, aspirin‐selenoesters, benzyl‐selenoesters, and hydroxy‐selenoesters could efficiently inhibit the biofilm production of the MRSA strain. It can be concluded that selenocompounds could act as efflux pump inhibitors, thus reducing the virulence of biofilm‐producing bacteria.}, keywords = {Selenium; multidrug resistance; biological activity; efflux pump; Biofilm}, year = {2024}, eissn = {1860-7187}, orcid-numbers = {Kincses, Annamária/0000-0002-1591-1419; Spengler, Gabriella/0000-0001-8085-0950} } @CONFERENCE{MTMT:35518286, title = {Evaluation of the potential of selenoesters to reverse multidrug resistance}, url = {https://m2.mtmt.hu/api/publication/35518286}, author = {Szemerédi, Nikoletta and Kincses, Annamária and Jitka, Viktorová and Enrique, Domínguez Álvarez and Spengler, Gabriella}, booktitle = {Magyar Mikrobiológiai Társaság 2024. évi Nagygyűlése/ Hungarian Society for Microbiology General Meeting 2024. - Absztraktok/ Abstracts}, unique-id = {35518286}, year = {2024}, pages = {28}, orcid-numbers = {Kincses, Annamária/0000-0002-1591-1419; Spengler, Gabriella/0000-0001-8085-0950} } @CONFERENCE{MTMT:35518284, title = {Drug repurposing strategy in bacterial infections: phenothiazine antipsychotics as efflux pump inhibitors}, url = {https://m2.mtmt.hu/api/publication/35518284}, author = {Nové, Márta and Rácz, Bálint and Kincses, Annamária and Spengler, Gabriella}, booktitle = {Magyar Mikrobiológiai Társaság 2024. évi Nagygyűlése/ Hungarian Society for Microbiology General Meeting 2024. - Absztraktok/ Abstracts}, unique-id = {35518284}, year = {2024}, pages = {26}, orcid-numbers = {Rácz, Bálint/0000-0003-0088-3408; Kincses, Annamária/0000-0002-1591-1419; Spengler, Gabriella/0000-0001-8085-0950} } @article{MTMT:35480474, title = {Structural and Solution Speciation Studies on fac -Tricarbonylrhenium(I) Complexes of 2,2′-Bipyridine Analogues}, url = {https://m2.mtmt.hu/api/publication/35480474}, author = {Pivarcsik, Tamás and Kljun, Jakob and Clemente Rodriguez, Sergio and Cortéz Alcaraz, David and Rapuš, Uroš and Nové, Márta and F. Várkonyi, Egon and Nyári, József and Bogdanov, Anita and Spengler, Gabriella and Turel, Iztok and Enyedy, Éva Anna}, doi = {10.1021/acsomega.4c07117}, journal-iso = {ACS OMEGA}, journal = {ACS OMEGA}, volume = {9}, unique-id = {35480474}, issn = {2470-1343}, year = {2024}, eissn = {2470-1343}, pages = {44601-44615}, orcid-numbers = {Bogdanov, Anita/0000-0003-3067-8835; Spengler, Gabriella/0000-0001-8085-0950; Turel, Iztok/0000-0001-6776-4062; Enyedy, Éva Anna/0000-0002-8058-8128} } @misc{MTMT:35417786, title = {Resistance reversing effect of azaindole and indole derivatives in bacteria}, url = {https://m2.mtmt.hu/api/publication/35417786}, author = {Szemerédi, Nikoletta and D., Hegedűs and Spengler, Gabriella and I., Szatmári}, unique-id = {35417786}, year = {2024}, orcid-numbers = {Spengler, Gabriella/0000-0001-8085-0950} } @misc{MTMT:35417782, title = {Selenocompounds as efflux pump and biofilm inhibitors on Staphylococcus aureus strains}, url = {https://m2.mtmt.hu/api/publication/35417782}, author = {Kincses, Annamária and Szemerédi, Nikoletta and M., Benito-Lama and Mosolygó, Tímea and D., Dózsai and Csonka, Ákos and E., Domínguez-Álvarez and Spengler, Gabriella}, unique-id = {35417782}, year = {2024}, orcid-numbers = {Kincses, Annamária/0000-0002-1591-1419; Mosolygó, Tímea/0000-0002-4499-388X; Spengler, Gabriella/0000-0001-8085-0950} } @article{MTMT:35201147, title = {Synthesis of Tumor Selective Indole and 8-Hydroxyquinoline Skeleton Containing Di-, or Triarylmethanes with Improved Cytotoxic Activity}, url = {https://m2.mtmt.hu/api/publication/35201147}, author = {Hegedűs, Dóra and Szemerédi, Nikoletta and Petrinca, Krisztina and Berkecz, Róbert and Spengler, Gabriella and Szatmári, István}, doi = {10.3390/molecules29174176}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {29}, unique-id = {35201147}, issn = {1420-3049}, abstract = {The reaction between glycine-type aminonaphthol derivatives substituted with 2- or 1-naphthol and indole or 7-azaindole has been tested. Starting from 2-naphthol as a precursor, the reaction led to the formation of ring-closed products, while in the case of a 1-naphthol-type precursor, the desired biaryl ester was isolated. The synthesis of a bifunctional precursor starting from 5-chloro-8-hydroxyquinoline, morpholine, and ethyl glyoxylate via modified Mannich reaction is reported. The formed Mannich base 10 was subjected to give bioconjugates with indole and 7-azaindole. The effect of the aldehyde component and the amine part of the Mannich base on the synthetic pathway was also investigated. In favor of having a preliminary overview of the structure-activity relationships, the derivatives have been tested on cancer and normal cell lines. In the case of bioconjugate 16, as the most powerful scaffold in the series bearing indole and a 5-chloro-8-hydroxyquinoline skeleton, a potent toxic activity against the resistant Colo320 colon adenocarcinoma cell line was observed. Furthermore, this derivative was selective towards cancer cell lines showing no toxicity on non-tumor fibroblast cells.}, year = {2024}, eissn = {1420-3049}, orcid-numbers = {Berkecz, Róbert/0000-0002-9076-2177; Spengler, Gabriella/0000-0001-8085-0950; Szatmári, István/0000-0002-8571-5229} } @article{MTMT:35156158, title = {Phytochemical Investigation of Carex praecox Schreb. and ACE-Inhibitory Activity of Oligomer Stilbenes of the Plant}, url = {https://m2.mtmt.hu/api/publication/35156158}, author = {Dávid, Csilla Zsuzsanna and Kúsz, Norbert and Agbadua, Orinamhe Godwin and Berkecz, Róbert and Kincses, Annamária and Spengler, Gabriella and Hunyadi, Attila and Hohmann, Judit and Vasas, Andrea}, doi = {10.3390/molecules29143427}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {29}, unique-id = {35156158}, issn = {1420-3049}, abstract = {Phenolic compounds are the main special metabolites of Cyperaceae species from phytochemical, pharmacological, and chemotaxonomical points of view. The present study focused on the isolation, structure determination, and pharmacological investigation of constituents from Carex praecox. Twenty-six compounds, including lignans, stilbenes, flavonoids, megastigmanes, chromenes, and phenylpropanoids, were identified from the methanol extract of the plant. Five of these compounds, namely, carexines A–E, are previously undescribed natural products. All compounds were isolated for the first time from C. praecox. The ACE-inhibitory activity of seven stilbenoid compounds was tested, and (–)-hopeaphenol proved to be the most active (IC50 7.7 ± 0.9 μM). The enzyme–kinetic studies revealed a mixed-type inhibition; therefore, domain-specific studies were also conducted. The in silico docking of (–)-hopeaphenol to the ACE affirmed some favorable interactions. In addition, the antiproliferative and antibacterial effects of some compounds were also evaluated.}, keywords = {Flavonoids; Lignans; STILBENES; Cyperaceae; ACE-inhibitory activity; Carex praecox}, year = {2024}, eissn = {1420-3049}, orcid-numbers = {Kúsz, Norbert/0000-0002-9973-6442; Berkecz, Róbert/0000-0002-9076-2177; Kincses, Annamária/0000-0002-1591-1419; Spengler, Gabriella/0000-0001-8085-0950; Hunyadi, Attila/0000-0003-0074-3472; Hohmann, Judit/0000-0002-2887-6392; Vasas, Andrea/0000-0002-1818-7702} } @article{MTMT:35135372, title = {pH-Triggered Hydrogel Nanoparticles for Efficient Anticancer Drug Delivery and Bioimaging Applications}, url = {https://m2.mtmt.hu/api/publication/35135372}, author = {Amin, Keristina and Imre-Deák, Ágota and Csanády, Miklós ifj. and Szemerédi, Nikoletta and Szabó, Diána and Turcsányi, Árpád and Ungor, Ditta Anita and Spengler, Gabriella and Rovó, László and Janovák, László}, doi = {10.3390/pharmaceutics16070931}, journal-iso = {PHARMACEUTICS}, journal = {PHARMACEUTICS}, volume = {16}, unique-id = {35135372}, issn = {1999-4923}, abstract = {In this work, we developed multifunctional hydrogel nanoparticles (NPs) that can encapsulate anticancer drugs and imaging contrast agents as well. Mitomycin C (MMC) and rhodamine B (RB) were selected as models for anticancer drugs and imaging contrasting agents, respectively. Both MMC and RB were linked to the succinated polyvinyl alcohol polymer (PVA-SA). The selected labeled hydrogel NPs ((0.5% RB)-PVA-SA NPs and (1.5% RB)-PVA-SA NPs) improved the RB quantum yield from 29.8% to a minimum of 42.7%. Moreover, they showed higher emission stability compared to free RB when they were repeatedly excited at 554 nm for 2 h. Furthermore, the dye polymeric interactions significantly increased the RB fluorescence lifetime by approximately twofold. All these optical properties pave the way for our labeled hydrogel NPs to be used in imaging-guided therapy. For the labeled MMC-loaded NPs, the MMC-binding efficiency was found to be exceedingly high in all synthesized samples: a minimum of 92% was achieved. In addition, the obtained pH-dependent drug release profiles as well as the cytotoxicity evaluation demonstrated the high potential of releasing MMC under acidic cancerous conditions. Moreover, the in vitro cellular uptake experiment confirmed the accumulation of MMC NPs throughout the cytoplasm.}, year = {2024}, eissn = {1999-4923}, orcid-numbers = {Imre-Deák, Ágota/0000-0002-6781-1727; Ungor, Ditta Anita/0000-0002-7659-0428; Spengler, Gabriella/0000-0001-8085-0950; Rovó, László/0000-0003-1782-1756; Janovák, László/0000-0002-2066-319X} } @article{MTMT:35084516, title = {Impact of V9302, a Competitive Antagonist of Transmembrane Glutamine Flux on Reversal of Resistance in Breast Cancer Cell Lines}, url = {https://m2.mtmt.hu/api/publication/35084516}, author = {Szemerédi, Nikoletta and Schelz, Zsuzsanna and Horváth, Dária Antónia and Rácz, Bálint and Szatmári, András G. and Abdallah, Hiba Faroug Muddather and Bózsity-Faragó, Noémi and Zupkó, István and Spengler, Gabriella}, doi = {10.3390/pharmaceutics16070877}, journal-iso = {PHARMACEUTICS}, journal = {PHARMACEUTICS}, volume = {16}, unique-id = {35084516}, issn = {1999-4923}, abstract = {Chemotherapy is a known treatment modality that improves the long-term survival of breast cancer patients. However, due to the resistance to numerous anticancer drugs, alternative chemotherapeutic strategies are required. Regarding antimetabolic drugs, several compounds have proven anticancer properties, such as statins. The present study aimed to investigate the in vitro effects of V9302, a competitive antagonist of glutamine flux, on different subtypes of breast cancers (estrogen, progesterone, and HER2 receptor-positive or negative, and Pgp-negative and Pgp-overexpressing). The interactions of V9302 with standard chemotherapeutic drugs (doxorubicin and cisplatin) were also determined by MTT staining on breast cancer cell lines. Furthermore, the influence of V9302 on the cell cycle of MCF-7 and its Pgp-overexpressing counterpart KCR was monitored by flow cytometry. It was shown that V9302 exerted synergistic interactions with doxorubicin in all breast cancer cell lines. In cell cycle analysis, the KCR cell line was more sensitive to V9302. After 48 h, cell proliferation was completely blocked, and elevated G1, suppressed S, and decreased G2/M could be detected. Inhibition of glutamate transport can be assumed to block resistance related to Pgp.}, year = {2024}, eissn = {1999-4923}, orcid-numbers = {Schelz, Zsuzsanna/0000-0002-8519-4830; Rácz, Bálint/0000-0003-0088-3408; Abdallah, Hiba Faroug Muddather/0000-0001-8472-330X; Zupkó, István/0000-0003-3243-5300; Spengler, Gabriella/0000-0001-8085-0950} }