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156 results on '"Kincses, Annamária"'

1. Seleno-vs. thioether triazine derivatives in search for new anticancer agents overcoming multidrug resistance in lymphoma

Author

Ali, Wesam, Garbo, Sabrina, Kincses, Annamária, Nové, Márta, Spengler, Gabriella, Di Bello, Elisabetta, Honkisz-Orzechowska, Ewelina, Karcz, Tadeusz, Szymańska, Ewa, Żesławska, Ewa, Starek, Małgorzata, Dąbrowska, Monika, Nitek, Wojciech, Kucwaj-Brysz, Katarzyna, Pyka, Patryk, Fioravanti, Rossella, Jacob, Claus, Battistelli, Cecilia, Zwergel, Clemens, and Handzlik, Jadwiga

Published
2022
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3. Phytochemical Investigation of Carex praecox Schreb. and ACE-Inhibitory Activity of Oligomer Stilbenes of the Plant.

Author

Dávid, Csilla Zsuzsanna, Kúsz, Norbert, Agbadua, Orinamhe Godwin, Berkecz, Róbert, Kincses, Annamária, Spengler, Gabriella, Hunyadi, Attila, Hohmann, Judit, and Vasas, Andrea

Subjects
MOLECULAR docking, PHENYLPROPANOIDS, LIGNANS, NATURAL products, PHENOLS
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. [ABSTRACT FROM AUTHOR]

Published
2024
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4. An insight into the structure of 5-spiro aromatic derivatives of imidazolidine-2,4-dione, a new group of very potent inhibitors of tumor multidrug resistance in T-lymphoma cells

Author

Żesławska, Ewa, Kucwaj-Brysz, Katarzyna, Kincses, Annamária, Spengler, Gabriella, Szymańska, Ewa, Czopek, Anna, Marć, Małgorzata Anna, Kaczor, Aneta, Nitek, Wojciech, Domínguez-Álvarez, Enrique, Latacz, Gniewomir, Kieć-Kononowicz, Katarzyna, and Handzlik, Jadwiga

Published
2021
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6. Discovery of phenylselenoether-hydantoin hybrids as ABCB1 efflux pump modulating agents with cytotoxic and antiproliferative actions in resistant T-lymphoma

Author

Ali, Wesam, Spengler, Gabriella, Kincses, Annamária, Nové, Márta, Battistelli, Cecilia, Latacz, Gniewomir, Starek, Małgorzata, Dąbrowska, Monika, Honkisz-Orzechowska, Ewelina, Romanelli, Annalisa, Rasile, Manuela Monica, Szymańska, Ewa, Jacob, Claus, Zwergel, Clemens, and Handzlik, Jadwiga

Published
2020
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17. Cyano- and Ketone-Containing Selenoesters as Multi-Target Compounds against Resistant Cancers

Author

Szemerédi, Nikoletta, primary, Dobiasová, Simona, additional, Salardón-Jiménez, Noemi, additional, Kincses, Annamária, additional, Nové, Márta, additional, Habibullah, Giyaullah, additional, Sevilla-Hernández, Clotilde, additional, Benito-Lama, Miguel, additional, Alonso-Martínez, Francisco-Javier, additional, Viktorová, Jitka, additional, Spengler, Gabriella, additional, and Domínguez-Álvarez, Enrique, additional

Published
2021
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22. Resistance modulating activity of selenoesters in bacteria

Author

Szeremedi, N., Kincses, Annamária, Rehorova, K., Viktorova, J., Domínguez-Álvarez, Enrique, and Spengler, G.

Abstract

Infections caused by multidrug resistant bacteria can lead to serious problems regarding the antibacterial therapy. Multidrug resistance (MDR) mechanisms allow resistant bacteria to have limited uptake of drugs, modification of their target molecules, drug inactivation, or release of the drug into the extracellular space by efflux pumps (EPs). Previously, selenoesters have proved to be effective derivatives with anticancer and antimicrobial activities. Based on these results, new selenoesters have been synthesized to achieve a more potent antibacterial activity. Thus, the quorum sensing inhibiting and antibiofilm effects in vitro of fifteen selenoesters (eight ketone-selenoesters and seven cyano-selenoesters) were investigated in this study. The minimum inhibitory concentrations (MICs) of the selenoesters were determined on sensitive and resistant Staphylococcus aureus strains. Biofilms produced by Pseudomonas aeruginosa (CCM, 3955) and S. aureus (ATCC, 25923) were used to evaluate the eruption of mature biofilm and the antibiofilm activity of the compounds. Additionally, two reference strains of Vibrio campbellii were used (BAA1118 and BAA1119) to establish the anti-quorum sensing activity of these novel selenoester derivatives. In this anti-quorum sensing assay, the viability of the cells and the quorum sensing inhibiting effects were determined in the presence of the selenoesters to differentiate between the toxic concentration and the quorum sensing inhibiting concentration. According to the screening of the antibacterial activity, the ketone-selenoesters resulted to be more potent antibacterial compounds than the cyano-selenoesters. The biofilm inhibitory capacity and the ability to disrupt mature biofilms of the derivatives were noteworthy in all the experimental systems considered. Regarding the QS inhibition, four ketone-selenoesters and three cyano-selenoesters among the tested compounds exerted a noteworthy effect on both V. campbellii BAA-1118 and BAA-1119 strains. The results obtained in this work point that these ketone- and cyano-selenoesters could be promising and valuable compounds in the search of novel antibacterials to combat the infections by resistant bacteria, as they have shown a promising anti-biofilm and anti-QS activity. Thus, seleniumcontaining compounds belonging to the family of the selenoester compounds could provide alternative and effective structural motifs to overcome bacterial MDR. Nevertheless, the mode of action of the compounds needs further investigation to be fully understood.

Published
2020

25. Efflux pump inhibition by symmetric selenoesters on colon adenocarcinoma cells

Author

Rácz, B., Kincses, Annamária, Benito-Lama, Miguel, González-Prádena, Ana, Domínguez-Álvarez, Enrique, and Spengler, Gabriella

Abstract

The development of resistance to chemotherapy in tumour cells is often due to altered membrane transport, such as the overexpression of ABCB1 (P-glycoprotein). Previously, selenium and its derivatives have been reported as antiproliferative, cytotoxic compounds that can also reduce drug resistance in tumour cells, trigger apoptotic events and enhance synergistically the anticancer activity of chemotherapy drugs such as doxorubicin. This work aims to elucidate how the symmetrical selenoesters exert their anticancer effect on sensitive and resistant human colon adenocarcinoma cells expressing ABCB1 protein. MTT assay was applied to assess both the antiproliferative and cytotoxic effects of the compounds on sensitive and resistant colon adenocarcinoma and normal embryonic lung fibroblast cells. A flow cytometry based assay which determines the accumulation of rhodamine 123 was used to assess the efflux pump inhibitory activity of the tested selenoesters. Finally, annexin V-FITC staining was used to determine the apoptosis-inducing effect of the most promising derivatives. Furthermore, the interaction of the compounds with doxorubicin was assessed by checkerboard combination assay and the type of interaction was calculated by Calcusyn software. Methyl ketone-containing compounds (EDAG-1, -5, -8) showed the most potent antiproliferative and cytotoxic effects. Out of them, EDAG-5 was the one that had the most synergistic interaction with doxorubicin. On the other hand, the methyloxycarbonylmethyl- and the methylcyano selenoesters had a very low cytotoxic activity on the normal MRC-5 fibroblast cell line. Methyl ketone- and methylcyano-selenoesters (EDAG-7, -10, 11) were more potent ABCB1 inhibitors than the reference compound verapamil. Finally, a methyl ketone selenoester (EDAG-1) was an effective inducer of apoptosis in the resistant Colo 320 cell line. The biological activities observed are comparable or higher than the ones determined in previous works. Thus, it seems that the inclusion of symmetric centres in these selenocompounds may favour (or at least retain) the biological activity. Based on these results, it can be concluded that these compounds (or derivatives containing these symmetrical elements) could be interesting scaffolds for future research in medicinal chemistry.

Published
2020

28. Antimicrobial, Anticancer and Multidrug-Resistant Reversing Activity of Novel Oxygen-, Sulfur- and Selenoflavones and Bioisosteric Analogues

Author

Marć, Małgorzata Anna, primary, Kincses, Annamária, additional, Rácz, Bálint, additional, Nasim, Muhammad Jawad, additional, Sarfraz, Muhammad, additional, Lázaro-Milla, Carlos, additional, Domínguez-Álvarez, Enrique, additional, Jacob, Claus, additional, Spengler, Gabriella, additional, and Almendros, Pedro, additional

Published
2020
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32. Synthesis, characterization, thermal properties and biological activity of diazine-ring containing hydrazones and their metal complexes

Author

Magyari, Józef, primary, Barta Holló, Berta, additional, Rodić, Marko V., additional, Jovanović, Ljiljana S., additional, Mészáros Szécsényi, Katalin, additional, Ferenc, Wiesława, additional, Osypiuk, Dariusz, additional, Mosolygó, Tímea, additional, Kincses, Annamária, additional, and Spengler, Gabriella, additional

Published
2020
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35. Salicylaldehyde thiosemicarbazone copper complexes: impact of hybridization with estrone on cytotoxicity, solution stability and redox activity

Author

Petrasheuskaya, Tatsiana V., primary, Kiss, Márton A., additional, Dömötör, Orsolya, additional, Holczbauer, Tamás, additional, May, Nóra V., additional, Spengler, Gabriella, additional, Kincses, Annamária, additional, Čipak Gašparović, Ana, additional, Frank, Éva, additional, and Enyedy, Éva A., additional

Published
2020
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38. Dually Acting Nonclassical 1,4-Dihydropyridines Promote the Anti-Tuberculosis (Tb) Activities of Clofazimine

Author

Lentz, Fabian, Reiling, Norbert, Spengler, Gabriella, Kincses, Annamária, Csonka, Andrea, Molnár, Joseph, and Hilgeroth, Andreas

Subjects
Dihydropyridines, Molecular Structure, synthesis, Communication, Spectrum Analysis, structure–activity, Antitubercular Agents, Drug Synergism, Microbial Sensitivity Tests, Mycobacterium tuberculosis, substituent, Clofazimine, inhibition, lcsh:QD241-441, antibacterial activity, lcsh:Organic chemistry, ATP Binding Cassette Transporter, Subfamily B, Member 1
Abstract

The number of effective antituberculotic drugs is strongly limited to four first-line drugs in standard therapy. In case of resistances second-line antibiotics are used with a poor efficacy and tolerability. Therefore, novel antituberculotic drugs are urgently needed. We synthesized novel nonclassical 1,4-dihydropyridines and evaluated their antituberculotic properties depending on substituent effects. Preferred substituents could be identified. As related classical 1,4-dihydropyridines are known as inhibitors of the transmembrane efflux pump ABCB1 in cancer cells, we wondered whether a use of our compounds may be of favour to enhance the antituberculotic drug efficacy of the second-line antituberculotic drug clofazimine, which is a known substrate of ABCB1 by a suggested inhibition of a corresponding efflux pump in Mycobacterium tuberculosis (Mtb). For this, we determined the ABCB1 inhibiting properties of our compounds in a mouse T-lymphoma cell line model and then evaluated the drug-enhancing properties of selected compounds in a co-application with clofazimine in our Mtb strain. We identified novel enhancers of clofazimine toxicity which could prevent clofazimine resistance development mediated by an efflux pump activity.

Published
2019

40. Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors

Author

Mosolygó, Tímea, primary, Kincses, Annamária, additional, Csonka, Andrea, additional, Tönki, Ádám Szabó, additional, Witek, Karolina, additional, Sanmartín, Carmen, additional, Marć, Małgorzata Anna, additional, Handzlik, Jadwiga, additional, Kieć-Kononowicz, Katarzyna, additional, Domínguez-Álvarez, Enrique, additional, and Spengler, Gabriella, additional

Published
2019
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43. Pronounced activity of aromatic selenocyanates against multidrug resistant ESKAPE bacteria

Author

Nasim, Muhammad Jawad, primary, Witek, Karolina, additional, Kincses, Annamária, additional, Abdin, Ahmad Yaman, additional, Żesławska, Ewa, additional, Marć, Małgorzata Anna, additional, Gajdács, Márió, additional, Spengler, Gabriella, additional, Nitek, Wojciech, additional, Latacz, Gniewomir, additional, Karczewska, Elżbieta, additional, Kieć-Kononowicz, Katarzyna, additional, Handzlik, Jadwiga, additional, and Jacob, Claus, additional

Published
2019
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45. The Role of Efflux Pumps and Environmental pH in Bacterial Multidrug Resistance.

Author

NOVÉ, MÁRTA, KINCSES, ANNAMÁRIA, MOLNÁR, JÓZSEF, AMARAL, LEONARD, and SPENGLER, GABRIELLA

Subjects
HYDROGEN-ion concentration, MULTIDRUG resistance, PROMETHAZINE, FLUORIMETRY, ESCHERICHIA coli
Abstract

Background/Aim: One of the most studied bacterial resistance mechanisms is the resistance related to multidrug efflux pumps. In our study the pump activity of the Escherichia coli K-12 AG100 strain expressing the AcrAB-TolC pump system was investigated at pH 7 and pH 5 in the presence of the efflux pump inhibitor (EPI) promethazine (PMZ). Materials and Methods: The EPI activity was assessed by real-time fluorimetry. The influence of PMZ treatment on the relative expression of the pump genes acrA, acrB and their regulators marA, marB, marR, the stress genes soxS, rob, as well as the bacterial growth control genes ftsI, and sdiA were determined by RT-qPCR. Results: The EPI activity of PMZ was more effective at neutral pH. The PMZ treatment induced a significant stress response in the bacterium at acidic pH by the up-regulation of genes. Conclusion: The genetic system that regulates the activity of the main efflux pump is pH-dependent. [ABSTRACT FROM AUTHOR]

Published
2020
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50. Interactions of Schiff base compounds and their coordination complexes with the drug cisplatin

Author

Magyari, József, primary, Barta Holló, Berta, additional, Vojinović-Ješić, Ljiljana S., additional, Radanović, Mirjana M., additional, Armaković, Stevan, additional, Armaković, Sanja J., additional, Molnár, Joseph, additional, Kincses, Annamária, additional, Gajdács, Márió, additional, Spengler, Gabriella, additional, and Mészáros Szécsényi, Katalin, additional

Published
2018
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