@article{MTMT:34840288, title = {A Novel 2-Methoxyestradiol Derivative: Disrupting Mitosis-Inhibiting Cell Motility and Inducing Apoptosis in HeLa Cells In Vitro}, url = {https://m2.mtmt.hu/api/publication/34840288}, author = {Njangiru, Isaac Kinyua and Bózsity-Faragó, Noémi and Resch, Vivien Erzsébet and Paragi, Gábor and Frank, Éva and Balogh, György Tibor and Zupkó, István and Minorics, Renáta}, doi = {10.3390/pharmaceutics16050622}, journal-iso = {PHARMACEUTICS}, journal = {PHARMACEUTICS}, volume = {16}, unique-id = {34840288}, issn = {1999-4923}, abstract = {The clinical application of 2-methoxyestradiol (2ME) in cancer therapy has been limited by its low solubility and rapid metabolism. Derivatives of 2ME have been synthesised to enhance bioavailability and decrease hepatic metabolism. Compound 4a, an analog of 2ME, has demonstrated exceptional pharmacological activity, in addition to promising pharmacokinetic profile. Our study, therefore, aimed at exploring the anticancer effects of 4a on the cervical cancer cell line, HeLa. Compound 4a exhibited a significant and dose-dependent antimetastatic and antiinvasive impact on HeLa cells, as determined by wound-healing and Boyden chamber assays, respectively. Hoechst/Propidium iodide (HOPI) double staining showcased a substantial induction of apoptosis via 4a, with minimal necrotic effect. Flow cytometry revealed a significant G2/M phase arrest, accompanied by a noteworthy rise in the sub-G1 cell population, indicating apoptosis, 18 h post-treatment. Moreover, a cell-independent tubulin polymerisation assay illustrated compound 4a’s ability to stabilise microtubules by promoting tubulin polymerisation. Molecular modelling experiments depicted that 4a interacts with the colchicine-binding site, nestled between the α and β tubulin dimers. Furthermore, 4a displayed an affinity for binding to and activating ER-α, as demonstrated by the luciferase reporter assay. These findings underscore the potential of 4a in inhibiting HPV18+ cervical cancer proliferation and cellular motility.}, year = {2024}, eissn = {1999-4923}, orcid-numbers = {Paragi, Gábor/0000-0001-5408-1748; Frank, Éva/0000-0002-1332-0551; Balogh, György Tibor/0000-0003-3347-1880; Zupkó, István/0000-0003-3243-5300; Minorics, Renáta/0000-0001-9685-813X} } @article{MTMT:34830192, title = {Immobilization of human tyrosine hydroxylase onto magnetic nanoparticles – A novel formulation of a therapeutic enzyme}, url = {https://m2.mtmt.hu/api/publication/34830192}, author = {Molnár, Zsófia Klára and Koplányi, Gábor and Farkas, Réka and Péli, Noémi and Kenéz, Balázs and Decsi, Balázs and Katona, Gábor and Balogh, György Tibor and Vértessy, Beáta (Grolmuszné) and Balogh Weiser, Diána}, doi = {10.1016/j.ijbiomac.2024.131939}, journal-iso = {INT J BIOL MACROMOL}, journal = {INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES}, volume = {268}, unique-id = {34830192}, issn = {0141-8130}, abstract = {Human tyrosine hydroxylase (hTH) has key role in the production of catecholamine neurotransmitters. The structure, function and regulation of hTH has been extensively researched area and the possibility of enzyme replacement therapy (ERT) involving hTH through nanocarriers has been raised as well. However, our understanding on how hTH may interact with nanocarriers is still lacking. In this work, we attempted to investigate the immobilization of hTH on magnetic nanoparticles (MNPs) with various surface linkers in quantitative and mechanistic detail. Our results showed that the activity of hTH was retained after immobilization via secondary and covalent interactions as well. The colloidal stability of hTH could be also enhanced proved by Dynamic light scattering and Zeta potential analysis and a homogenous enzyme layer could be achieved, which was investigated by Raman mapping. The covalent attachment of hTH on MNPs via aldehyde or epoxy linkers provide irreversible immobilization and 38.1 % and 16.5 % recovery (ER). The hTH-MNPs catalyst had 25 % ER in average in simulated nasal electrolyte solution (SNES). This outcome highlights the relevance of immobilization applying MNPs as a potential formulation tool of sensitive therapeutic enzymes offering new opportunities for ERT related to neurodegenerative disorders. © 2024 The Author(s)}, year = {2024}, eissn = {1879-0003}, orcid-numbers = {Koplányi, Gábor/0000-0002-3791-1057; Katona, Gábor/0000-0003-1564-4813; Balogh, György Tibor/0000-0003-3347-1880; Balogh Weiser, Diána/0000-0002-9957-1203} } @article{MTMT:34779108, title = {Diterpenes Isolated from Three Different Plectranthus Sensu Lato Species and Their Antiproliferative Activities against Gynecological and Glioblastoma Cancer Cells}, url = {https://m2.mtmt.hu/api/publication/34779108}, author = {Gáborová, Mária and Vágvölgyi, Máté and Tayeb, Bizhar Ahmed and Minorics, Renáta and Zupkó, István and Jurček, Ondřej and Béni, Szabolcs and Kubínová, Renata and Balogh, György Tibor and Hunyadi, Attila}, doi = {10.1021/acsomega.4c00800}, journal-iso = {ACS OMEGA}, journal = {ACS OMEGA}, volume = {9}, unique-id = {34779108}, issn = {2470-1343}, year = {2024}, eissn = {2470-1343}, pages = {18495-18504}, orcid-numbers = {Vágvölgyi, Máté/0000-0002-2233-9422; Tayeb, Bizhar Ahmed/0000-0001-5197-564X; Minorics, Renáta/0000-0001-9685-813X; Zupkó, István/0000-0003-3243-5300; Béni, Szabolcs/0000-0001-7056-6825; Balogh, György Tibor/0000-0003-3347-1880; Hunyadi, Attila/0000-0003-0074-3472} } @article{MTMT:34538437, title = {A Comparative Pharmacokinetic Study for Cysteamine-Containing Eye Drops as an Orphan Topical Therapy in Cystinosis}, url = {https://m2.mtmt.hu/api/publication/34538437}, author = {Csorba, Anita and Katona, Gábor and Budai-Szűcs, Mária and Balogh Weiser, Diána and Molnár, P. and Maka, Erika and Nochta-Kazsoki, Adrienn Katalin and Vajna, Márton Antal and Zelkó, Romána and Nagy, Zoltán Zsolt and Balogh, György Tibor}, doi = {10.3390/ijms25031623}, journal-iso = {INT J MOL SCI}, journal = {INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES}, volume = {25}, unique-id = {34538437}, issn = {1661-6596}, year = {2024}, eissn = {1422-0067}, orcid-numbers = {Csorba, Anita/0000-0002-3256-9440; Katona, Gábor/0000-0003-1564-4813; Budai-Szűcs, Mária/0000-0001-5187-5702; Balogh Weiser, Diána/0000-0002-9957-1203; Maka, Erika/0000-0002-3631-3506; Nochta-Kazsoki, Adrienn Katalin/0000-0002-0611-3124; Vajna, Márton Antal/0000-0001-5280-7533; Zelkó, Romána/0000-0002-5419-9137; Nagy, Zoltán Zsolt/0000-0002-7330-0464; Balogh, György Tibor/0000-0003-3347-1880} } @article{MTMT:34225112, title = {Development of innovative electrospun nepafenac-loaded nanofibers-based ophthalmic inserts}, url = {https://m2.mtmt.hu/api/publication/34225112}, author = {Safaa, Mohammed Omer and Nagy, Nándor and Szőcs, Emőke and Kádár, Szabina and Völgyi, Gergely and Pinke, Balázs and Mészáros, László and Katona, Gábor and Vincze, Anna and Dormán, Péter and Nagy, Zoltán Zsolt and Balogh, György Tibor and Nochta-Kazsoki, Adrienn Katalin and Zelkó, Romána}, doi = {10.1016/j.ijpharm.2023.123554}, journal-iso = {INT J PHARM}, journal = {INTERNATIONAL JOURNAL OF PHARMACEUTICS}, volume = {647}, unique-id = {34225112}, issn = {0378-5173}, year = {2023}, eissn = {1873-3476}, orcid-numbers = {Safaa, Mohammed Omer/0000-0003-4212-9147; Nagy, Nándor/0000-0002-6223-5214; Völgyi, Gergely/0000-0001-8990-3916; Pinke, Balázs/0000-0002-6683-6199; Mészáros, László/0000-0001-5979-7403; Katona, Gábor/0000-0003-1564-4813; Nagy, Zoltán Zsolt/0000-0002-7330-0464; Balogh, György Tibor/0000-0003-3347-1880; Nochta-Kazsoki, Adrienn Katalin/0000-0002-0611-3124; Zelkó, Romána/0000-0002-5419-9137} } @CONFERENCE{MTMT:34165281, title = {In vitro and ex vivo test systems in the development of cyclodextrin-enabled eye drops}, url = {https://m2.mtmt.hu/api/publication/34165281}, author = {Vincze, Anna and Balogh, György Tibor}, booktitle = {EUROCD 2023 7th European Cyclodextrin Conference}, unique-id = {34165281}, year = {2023}, orcid-numbers = {Balogh, György Tibor/0000-0003-3347-1880} } @CONFERENCE{MTMT:34163444, title = {Ginkgo biloba EGb 761® extract in vitro permeability study}, url = {https://m2.mtmt.hu/api/publication/34163444}, author = {Erdős, Dóra and D. Marton, András and Balogh, György Tibor}, booktitle = {EUROCD 2023 7th European Cyclodextrin Conference}, unique-id = {34163444}, year = {2023}, orcid-numbers = {Balogh, György Tibor/0000-0003-3347-1880} } @article{MTMT:34147665, title = {Medicinal Chemistry‐driven Approach to Novel 2‐Substituted Benzoxazole – Estradiol Chimeras: Synthesis, Anticancer Activity and Early ADME Profile}, url = {https://m2.mtmt.hu/api/publication/34147665}, author = {Kovács, Ferenc and Huliák, Ildikó and Árva, Hédi and Csontné Kiricsi, Mónika and Erdős, Dóra and Kocsis, Marianna and Takács, Gergely and Balogh, György Tibor and Nagyné Frank, Éva}, doi = {10.1002/cmdc.202300352}, journal-iso = {CHEMMEDCHEM}, journal = {CHEMMEDCHEM}, volume = {18}, unique-id = {34147665}, issn = {1860-7179}, abstract = {The efficient synthesis of novel estradiol‐based A‐ring‐fused oxazole derivatives, which can be considered as benzoxazole‐steroid domain‐integrated hybrids containing a common benzene structural motif, is described. The target compounds were prepared from steroidal 2‐aminophenol precursors by heterocycle formation or functional group interconversion (FGI) strategies. According to 2D projection‐based t‐distributed stochastic neighbor embedding (t‐SNE), the novel molecules were proved to represent a new chemical space among steroid drugs. They were characterized based on critical physicochemical parameters using in silico and experimental data. The performance of the compounds to inhibit cell proliferation was tested on four human cancer cell lines and non‐cancerous cells. Further examinations were performed to reveal IC50 and lipophilic ligand efficiency (LLE) values, cancer cell selectivity, and apoptosis‐triggering features. Pharmacological tests and LLE metric revealed that some derivatives, especially the 2‐(4‐ethylpiperazin‐1‐yl)oxazole derivative exhibit strong anticancer activity and trigger the apoptosis of cancer cells with relatively low promiscuity risk similarly to the structurally most closely‐related and intensively studied anticancer agent, 2‐methoxy‐estradiol.}, year = {2023}, eissn = {1860-7187}, orcid-numbers = {Csontné Kiricsi, Mónika/0000-0002-8416-2052; Balogh, György Tibor/0000-0003-3347-1880; Nagyné Frank, Éva/0000-0002-1332-0551} } @article{MTMT:34146936, title = {Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB Transport}, url = {https://m2.mtmt.hu/api/publication/34146936}, author = {Juhász, Ádám and Ungor, Ditta Anita and Varga, Norbert and Katona, Gábor and Balogh, György Tibor and Csapó, Edit}, doi = {10.3390/ijms241814251}, journal-iso = {INT J MOL SCI}, journal = {INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES}, volume = {24}, unique-id = {34146936}, issn = {1661-6596}, abstract = {Encapsulation possibilities of an extensively investigated neuroprotective drug (kynurenic acid, KYNA) are studied via lipid-based nanocarriers to increase the blood–brain barrier (BBB) specific permeability. The outcomes of various preparation conditions such as stirring and sonication time, concentration of the lipid carriers and the drug, and the drug-to-lipid ratio are examined. Considering the experimentally determined encapsulation efficiency, hydrodynamic diameter, and ζ-potential values, the initial lipid and drug concentration as well as the stirring and sonication time of the preparation were optimized. The average hydrodynamic diameter of the prepared asolectin-(LIP) and water-soluble lipopolymer (WSLP)-based liposomes was found to be ca. 25 and 60 nm under physiological conditions. The physicochemical characterization of the colloidal carriers proves that the preparation of the drug-loaded liposomes was a successful process, and secondary interactions were indicated between the drug molecule and the polymer residues around the WSLP membrane. Dissolution profiles of the active molecule under physiological conditions were registered, and the release of the unformulated and encapsulated drug is very similar. In addition to this outcome, the in vitro polar brain lipid extract (porcine)-based permeability test proved the achievement of two- or fourfold higher BBB specific penetration and lipid membrane retention for KYNA in the liposomal carriers relative to the unformatted drug.}, year = {2023}, eissn = {1422-0067}, orcid-numbers = {Juhász, Ádám/0000-0003-0033-7968; Ungor, Ditta Anita/0000-0002-7659-0428; Varga, Norbert/0000-0002-9667-6608; Katona, Gábor/0000-0003-1564-4813; Balogh, György Tibor/0000-0003-3347-1880; Csapó, Edit/0000-0002-6980-9524} } @article{MTMT:34119941, title = {DIY Virtual Chemical Libraries - Novel Starting Points for Drug Discovery}, url = {https://m2.mtmt.hu/api/publication/34119941}, author = {Takács, Gergely and Havasi, Dávid and Sándor, Márk and Dohánics, Zsolt and Balogh, György Tibor and Kiss, Róbert}, doi = {10.1021/acsmedchemlett.3c00146}, journal-iso = {ACS MED CHEM LETT}, journal = {ACS MEDICINAL CHEMISTRY LETTERS}, volume = {14}, unique-id = {34119941}, issn = {1948-5875}, year = {2023}, pages = {1188-1197}, orcid-numbers = {Havasi, Dávid/0000-0003-3366-4009; Balogh, György Tibor/0000-0003-3347-1880} }