TY - JOUR AU - Kincses, Annamária AU - Szemerédi, Nikoletta AU - Benito‐Lama, Miguel AU - Dózsai, Dávid AU - Csonka, Ákos AU - Domínguez‐Álvarez, Enrique AU - Spengler, Gabriella TI - Selenocompounds as Potent Efflux Pump Inhibitors on Gram‐positive Bacteria JF - CHEMMEDCHEM J2 - CHEMMEDCHEM PY - 2024 SN - 1860-7179 DO - 10.1002/cmdc.202400691 UR - https://m2.mtmt.hu/api/publication/35594147 ID - 35594147 AB - 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. LA - English DB - MTMT ER - TY - CONF AU - Szemerédi, Nikoletta AU - Kincses, Annamária AU - Jitka, Viktorová AU - Enrique, Domínguez Álvarez AU - Spengler, Gabriella TI - Evaluation of the potential of selenoesters to reverse multidrug resistance T2 - Magyar Mikrobiológiai Társaság 2024. évi Nagygyűlése/ Hungarian Society for Microbiology General Meeting 2024. - Absztraktok/ Abstracts C1 - Siófok PY - 2024 SP - 28 UR - https://m2.mtmt.hu/api/publication/35518286 ID - 35518286 N1 - Abstracts LA - English DB - MTMT ER - TY - CONF AU - Nové, Márta AU - Rácz, Bálint AU - Kincses, Annamária AU - Spengler, Gabriella TI - Drug repurposing strategy in bacterial infections: phenothiazine antipsychotics as efflux pump inhibitors T2 - Magyar Mikrobiológiai Társaság 2024. évi Nagygyűlése/ Hungarian Society for Microbiology General Meeting 2024. - Absztraktok/ Abstracts C1 - Siófok PY - 2024 SP - 26 UR - https://m2.mtmt.hu/api/publication/35518284 ID - 35518284 N1 - Abstracts LA - English DB - MTMT ER - TY - JOUR AU - Pivarcsik, Tamás AU - Kljun, Jakob AU - Clemente Rodriguez, Sergio AU - Cortéz Alcaraz, David AU - Rapuš, Uroš AU - Nové, Márta AU - F. Várkonyi, Egon AU - Nyári, József AU - Bogdanov, Anita AU - Spengler, Gabriella AU - Turel, Iztok AU - Enyedy, Éva Anna TI - Structural and Solution Speciation Studies on fac -Tricarbonylrhenium(I) Complexes of 2,2′-Bipyridine Analogues JF - ACS OMEGA J2 - ACS OMEGA VL - 9 PY - 2024 IS - 44 SP - 44601 EP - 44615 PG - 15 SN - 2470-1343 DO - 10.1021/acsomega.4c07117 UR - https://m2.mtmt.hu/api/publication/35480474 ID - 35480474 LA - English DB - MTMT ER - TY - GEN AU - Szemerédi, Nikoletta AU - D., Hegedűs AU - Spengler, Gabriella AU - I., Szatmári TI - Resistance reversing effect of azaindole and indole derivatives in bacteria CY - 2024. 04. 27-30 PY - 2024 UR - https://m2.mtmt.hu/api/publication/35417786 ID - 35417786 LA - English DB - MTMT ER - TY - GEN AU - Kincses, Annamária AU - Szemerédi, Nikoletta AU - M., Benito-Lama AU - Mosolygó, Tímea AU - D., Dózsai AU - Csonka, Ákos AU - E., Domínguez-Álvarez AU - Spengler, Gabriella TI - Selenocompounds as efflux pump and biofilm inhibitors on Staphylococcus aureus strains CY - 2024. 04. 27-30. PY - 2024 UR - https://m2.mtmt.hu/api/publication/35417782 ID - 35417782 LA - English DB - MTMT ER - TY - JOUR AU - Hegedűs, Dóra AU - Szemerédi, Nikoletta AU - Petrinca, Krisztina AU - Berkecz, Róbert AU - Spengler, Gabriella AU - Szatmári, István TI - Synthesis of Tumor Selective Indole and 8-Hydroxyquinoline Skeleton Containing Di-, or Triarylmethanes with Improved Cytotoxic Activity JF - MOLECULES J2 - MOLECULES VL - 29 PY - 2024 IS - 17 PG - 14 SN - 1420-3049 DO - 10.3390/molecules29174176 UR - https://m2.mtmt.hu/api/publication/35201147 ID - 35201147 N1 - Institute of Pharmaceutical Chemistry, University of Szeged, Eötvös u. 6, Szeged, H-6720, Hungary Department of Medical Microbiology, Albert Szent-Györgyi Health Center, Albert Szent-Györgyi Medical School, University of Szeged, Semmelweis utca 6, Szeged, H-6725, Hungary Institute of Pharmaceutical Analysis, University of Szeged, Somogyi u. 4, Szeged, H-6720, Hungary Department of Forensic Medicine, Albert Szent-Györgyi Health Center, Kossuth Lajos sgt. 40, Szeged, H-6724, Hungary HUN-REN–SZTE Stereochemistry Research Group, University of Szeged, Eötvös u. 6, Szeged, H-6720, Hungary Export Date: 24 September 2024 CODEN: MOLEF Correspondence Address: Szatmári, I.; Institute of Pharmaceutical Chemistry, Eötvös u. 6, Hungary; email: szatmari.istvan@szte.hu Chemicals/CAS: 8 quinolinol, 148-24-3; indole, 120-72-9; methane, 74-82-8; Antineoplastic Agents; indole; Indoles; Methane; Oxyquinoline Funding details: Innovációs és Technológiai Minisztérium Funding details: Hungarian Scientific Research Fund, OTKA, K-138871 Funding details: Hungarian Scientific Research Fund, OTKA Funding details: TKP-2021-EGA-32, ÚNKP-23-4-SZTE-347 Funding details: Magyar Tudományos Akadémia, MTA, ÚNKP-23-5-SZTE-677 Funding details: Magyar Tudományos Akadémia, MTA Funding details: Nemzeti Kutatási, Fejlesztési és Innovaciós Alap, NKFIA, BO/00158/22/5 Funding details: Nemzeti Kutatási, Fejlesztési és Innovaciós Alap, NKFIA Funding text 1: The authors thank the Hungarian Research Foundation (OTKA No. K-138871), the Ministry of Human Capacities, Hungary grant, TKP-2021-EGA-32. N.S. was supported by the \\u00DANKP-23-4-SZTE-347 New National Excellence Program of the Ministry for Innovation and Technology from the source of the National Research, Development and Innovation Fund. G.S. was supported by the J\\u00E1nos Bolyai Research Scholarship (BO/00158/22/5) of the Hungarian Academy of Sciences and by the \\u00DANKP-23-5-SZTE-677 New National Excellence Program of the Ministry for Culture and Innovation from the source of the National Research, Development and Innovation Fund. The FTIR analysis was performed by \\u00C9va Anna Enyedy. AB - 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. LA - English DB - MTMT ER - TY - JOUR AU - Dávid, Csilla Zsuzsanna AU - Kúsz, Norbert AU - Agbadua, Orinamhe Godwin AU - Berkecz, Róbert AU - Kincses, Annamária AU - Spengler, Gabriella AU - Hunyadi, Attila AU - Hohmann, Judit AU - Vasas, Andrea TI - Phytochemical Investigation of Carex praecox Schreb. and ACE-Inhibitory Activity of Oligomer Stilbenes of the Plant JF - MOLECULES J2 - MOLECULES VL - 29 PY - 2024 IS - 14 PG - 19 SN - 1420-3049 DO - 10.3390/molecules29143427 UR - https://m2.mtmt.hu/api/publication/35156158 ID - 35156158 N1 - Department of Pharmacognosy, University of Szeged, Szeged, 6720, Hungary Institute of Pharmaceutical Analysis, University of Szeged, Szeged, 6720, Hungary HUN-REN-USZ Biologically Active Natural Products Research Group, University of Szeged, Eötvös u. 6, Szeged, 6720, Hungary Department of Medical Microbiology, Albert Szent-Györgyi Health Center, Albert Szent-Györgyi Medical School, University of Szeged, Szeged, 6725, Hungary Cited By :1 Export Date: 3 October 2024 CODEN: MOLEF Correspondence Address: Vasas, A.; Department of Pharmacognosy, Hungary; email: vasas.andrea@szte.hu Chemicals/CAS: Angiotensin-Converting Enzyme Inhibitors; Anti-Bacterial Agents; hopeaphenol; Phenols; Phytochemicals; Plant Extracts; Stilbenes Funding details: National Research, Development and Innovation Office Funding details: Emberi Eroforrások Minisztériuma, EMMI, UNKP-21-3 Funding details: Emberi Eroforrások Minisztériuma, EMMI Funding details: K-135845, K-134704 Funding details: TKP2021-EGA-32 Funding text 1: This research was funded by the National Research, Development and Innovation Office, Hungary (NKFIH; K-135845 and K-134704), and the Ministry of Innovation and Technology of Hungary from NKFIH Fund, project no. TKP2021-EGA-32. Funding text 2: Support from the New National Excellence Program of the Ministry of Human Capacities [UNKP-21-3 (C.Z.D.)] is gratefully acknowledged. AB - 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. LA - English DB - MTMT ER - TY - JOUR AU - Amin, Keristina AU - Imre-Deák, Ágota AU - Csanády, Miklós ifj. AU - Szemerédi, Nikoletta AU - Szabó, Diána AU - Turcsányi, Árpád AU - Ungor, Ditta Anita AU - Spengler, Gabriella AU - Rovó, László AU - Janovák, László TI - pH-Triggered Hydrogel Nanoparticles for Efficient Anticancer Drug Delivery and Bioimaging Applications JF - PHARMACEUTICS J2 - PHARMACEUTICS VL - 16 PY - 2024 IS - 7 PG - 19 SN - 1999-4923 DO - 10.3390/pharmaceutics16070931 UR - https://m2.mtmt.hu/api/publication/35135372 ID - 35135372 AB - 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. LA - English DB - MTMT ER - TY - JOUR AU - Szemerédi, Nikoletta AU - Schelz, Zsuzsanna AU - Horváth, Dária Antónia AU - Rácz, Bálint AU - Szatmári, András G. AU - Abdallah, Hiba Faroug Muddather AU - Bózsity-Faragó, Noémi AU - Zupkó, István AU - Spengler, Gabriella TI - Impact of V9302, a Competitive Antagonist of Transmembrane Glutamine Flux on Reversal of Resistance in Breast Cancer Cell Lines JF - PHARMACEUTICS J2 - PHARMACEUTICS VL - 16 PY - 2024 IS - 7 PG - 14 SN - 1999-4923 DO - 10.3390/pharmaceutics16070877 UR - https://m2.mtmt.hu/api/publication/35084516 ID - 35084516 N1 - Funding: This research was funded by the Albert Szent-Györgyi Medical School, University of Szeged, Hungary, grant number: SZTESZAOK-KKASZGYA2023/5S772; by the Hungarian National Science and Research Fund (OTKA), grant No. 143690; by the Ministry of Innovation and Technology of Hungary from the National Research, Development, and Innovation Fund project no. TKP2021-EGA-32. G.S. was supported by the János Bolyai research Scholarship (BO/00158/22/5) of theHungarian Academy of Sciences. AB - 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. LA - English DB - MTMT ER -