@article{MTMT:34172544, title = {Highly Selective MIF Ketonase Inhibitor KRP-6 Diminishes M1 Macrophage Polarization and Metabolic Reprogramming}, url = {https://m2.mtmt.hu/api/publication/34172544}, author = {Vámos, Eszter and Kálmán, Nikoletta and Sturm, Eva Maria and Nayak, Barsha Baisakhi and Teppan, Julia and Bagóné Vántus, Viola and Kovács, Dominika and Makszin, Lilla and Lóránd, Tamás and Gallyas, Ferenc and Radnai, Balázs}, doi = {10.3390/antiox12101790}, journal-iso = {ANTIOXIDANTS-BASEL}, journal = {ANTIOXIDANTS}, volume = {12}, unique-id = {34172544}, abstract = {Macrophage polarization is highly involved in autoimmunity. M1 polarized macrophages drive inflammation and undergo metabolic reprogramming, involving downregulation of mitochondrial energy production and acceleration of glycolysis. Macrophage migration inhibitory factor (MIF), an enigmatic tautomerase (ketonase and enolase), was discovered to regulate M1 polarization. Here, we reveal that KRP-6, a potent and highly selective MIF ketonase inhibitor, reduces MIF-induced human blood eosinophil and neutrophil migration similarly to ISO-1, the most investigated tautomerase inhibitor. We equally discovered that KRP-6 prevents M1 macrophage polarization and reduces ROS production in IFN-γ-treated cells. During metabolic reprogramming, KRP-6 improved mitochondrial bioenergetics by ameliorating basal respiration, ATP production, coupling efficiency and maximal respiration in LPS+IFN-γ-treated cells. KRP-6 also reduced glycolytic flux in M1 macrophages. Moreover, the selective MIF ketonase inhibitor attenuated LPS+IFN-γ-induced downregulation of PARP-1 and PARP-2 mRNA expression. We conclude that KRP-6 represents a promising novel therapeutic compound for autoimmune diseases, which strongly involves M1 macrophage polarization.}, year = {2023}, eissn = {2076-3921}, orcid-numbers = {Vámos, Eszter/0000-0003-0622-442X; Makszin, Lilla/0000-0002-9764-4763; Gallyas, Ferenc/0000-0002-1906-4333} } @article{MTMT:33546311, title = {Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice}, url = {https://m2.mtmt.hu/api/publication/33546311}, author = {Garai, János and Radnai, Balázs and Vámos, Eszter and Kovács, Dominika and Bagóné Vántus, Viola and Rumbus, Zoltán and Pákai, Eszter and Garami, András and Gulyás, Gergely and Agócs, Attila and Krekó, Marcell and Zaman, K. and Prókai, L. and Őrfi, László and Jakus, Péter and Lóránd, Tamás}, doi = {10.1016/j.ejmech.2022.115050}, journal-iso = {EUR J MED CHEM}, journal = {EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY}, volume = {247}, unique-id = {33546311}, issn = {0223-5234}, year = {2023}, eissn = {1768-3254}, orcid-numbers = {Vámos, Eszter/0000-0003-0622-442X; Garami, András/0000-0003-2493-0571; Krekó, Marcell/0000-0002-4972-972X; Őrfi, László/0000-0001-6149-2385} } @article{MTMT:33090617, title = {Heterociklusos vegyületek szintézise a Pécsi Tudományegyetem Orvosi Kémiai Intézetében}, url = {https://m2.mtmt.hu/api/publication/33090617}, author = {Lóránd, Tamás and Perjési, Pál}, doi = {10.24100/MKF.2022.02.92}, journal-iso = {MAGY KÉM FOLY KÉM KÖZL}, journal = {MAGYAR KÉMIAI FOLYÓIRAT - KÉMIAI KÖZLEMÉNYEK (1997-)}, volume = {128}, unique-id = {33090617}, issn = {1418-9933}, year = {2022}, eissn = {1418-8600}, pages = {92-101}, orcid-numbers = {Perjési, Pál/0000-0002-1057-9664} } @{MTMT:32131103, title = {The role of the macrophage migration inhibitory factor in lipopolysaccharide-induced hypothermia in mice}, url = {https://m2.mtmt.hu/api/publication/32131103}, author = {Rumbus, Zoltán and Garai, János and Kéringer, Patrik and Radnai, Balázs and Lóránd, Tamás and Garami, András}, booktitle = {Medical Conference for PhD Students and Experts of Clinical Sciences 2021}, unique-id = {32131103}, year = {2021}, pages = {115-115}, orcid-numbers = {Garami, András/0000-0003-2493-0571} } @article{MTMT:32095838, title = {Tetralone derivatives are MIF tautomerase inhibitors and attenuate macrophage activation and amplify the hypothermic response in endotoxemic mice}, url = {https://m2.mtmt.hu/api/publication/32095838}, author = {Garai, János and Krekó, Marcell and Őrfi, László and Jakus, Péter and Rumbus, Zoltán and Kéringer, Patrik and Garami, András and Vámos, Eszter and Kovács, Dominika and Bagóné Vántus, Viola and Radnai, Balázs and Lóránd, Tamás}, doi = {10.1080/14756366.2021.1916010}, journal-iso = {J ENZYM INHIB MED CH}, journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY}, volume = {36}, unique-id = {32095838}, issn = {1475-6366}, year = {2021}, eissn = {1475-6374}, pages = {1357-1369}, orcid-numbers = {Krekó, Marcell/0000-0002-4972-972X; Őrfi, László/0000-0001-6149-2385; Rumbus, Zoltán/0000-0003-2898-6628; Garami, András/0000-0003-2493-0571; Vámos, Eszter/0000-0003-0622-442X} } @{MTMT:31839932, title = {ULTRA-VIOLET AND INFRARED SPECTROSCOPY OF CHALCONES AND CYCLIC CHALCONE ANALOGS. EFFECT OF THE RING SIZE AND THE SUBSTITUENTS}, url = {https://m2.mtmt.hu/api/publication/31839932}, author = {Lóránd, Tamás and Kulcsár, Győző and Petra, Horváth and Perjési, Pál}, booktitle = {Chalcones and their synthetic analogs}, unique-id = {31839932}, year = {2020}, pages = {57-92}, orcid-numbers = {Kulcsár, Győző/0000-0002-4098-1072; Perjési, Pál/0000-0002-1057-9664} } @article{MTMT:31155279, title = {Study on the Synthesis, Antioxidant Properties, and Self-Assembly of Carotenoid–Flavonoid Conjugates}, url = {https://m2.mtmt.hu/api/publication/31155279}, author = {Linzembold, Ildikó Erzsébet and Czett, Dalma and Böddi, Katalin and Kurtán, Tibor and Király, Sándor Balázs and Gulyás, Gergely and Takátsy, Anikó and Lóránd, Tamás and Deli, József and Agócs, Attila and Nagy, Veronika}, doi = {10.3390/molecules25030636}, journal-iso = {MOLECULES}, journal = {MOLECULES}, volume = {25}, unique-id = {31155279}, issn = {1420-3049}, abstract = {Flavonoids and carotenoids possess beneficial physiological effects, such as high antioxidant capacity, anticarcinogenic, immunomodulatory, and anti-inflammatory properties, as well as protective effects against UV light. The covalent coupling of hydrophobic carotenoids with hydrophilic flavonoids, such as daidzein and chrysin, was achieved, resulting in new amphipathic structures. 7-Azidohexyl ethers of daidzein and chrysin were prepared in five steps, and their azide-alkyne [4 + 2] cycloaddition with pentynoates of 80-apo-β-carotenol, zeaxanthin, and capsanthin afforded carotenoid–flavonoid conjugates. The trolox-equivalent antioxidant capacity against ABTS•+ radical cation and self-assembly of the final products were examined. The 1:1 flavonoid–carotenoid hybrids generally showed higher antioxidant activity than their parent flavonoids but lower than that of the corresponding carotenoids. The diflavonoid hybrids of zeaxanthin and capsanthin, however, were found to exhibit a synergistic enhancement in antioxidant capacities. ECD (electronic circular dichroism) and UV-vis analysis of zeaxanthin–flavonoid conjugates revealed that they form different optically active J-aggregates in acetone/water and tetrahydrofuran/water mixtures depending on the solvent ratio and type of the applied aprotic polar solvent, while the capsanthin derivatives showed no self-assembly. The zeaxanthin bis-triazole conjugates with daidzein and with chrysin, differing only in the position of a phenolic hydroxyl group, showed significantly different aggregation profile upon the addition of water.}, keywords = {Flavonoids; carotenoids; antioxidant capacity; Electronic circular dichroism; Click-reaction; supramolecular chirality; zeaxanthin–flavonoid conjugates}, year = {2020}, eissn = {1420-3049}, orcid-numbers = {Deli, József/0000-0002-0625-6117; Nagy, Veronika/0000-0002-9019-7980} } @article{MTMT:30758489, title = {Novel cell wall antifungals reveal a special synergistic activity in pbr1 mutants resistant to the glucan synthesis antifungals papulacandins and echinocandins}, url = {https://m2.mtmt.hu/api/publication/30758489}, author = {Berzaghi, R. and Agócs, Attila and Gulyás, Gergely and Kocsis, Béla and Ribas, J.C. and Lóránd, Tamás}, doi = {10.3389/fmicb.2019.01692}, journal-iso = {FRONT MICROBIOL}, journal = {FRONTIERS IN MICROBIOLOGY}, volume = {10}, unique-id = {30758489}, issn = {1664-302X}, year = {2019}, eissn = {1664-302X} } @article{MTMT:3252956, title = {Mannich Ketones as Possible Antimycobacterial Agents.}, url = {https://m2.mtmt.hu/api/publication/3252956}, author = {Lutz, Z and Orban, K and Bóna, Ágnes and Márk, László and Maász, Gábor and Prókai, László and Seress, László and Lóránd, Tamás}, doi = {10.1002/ardp.201700102}, journal-iso = {ARCH PHARM}, journal = {ARCHIV DER PHARMAZIE}, volume = {350}, unique-id = {3252956}, issn = {0365-6233}, abstract = {Twenty-three known unsaturated and fused Mannich ketones and their reduced derivatives (amino alcohols) were selected for an antituberculotic study. They were screened against several mycobacterial strains including Mycobacterium tuberculosis, M. xenopi, and M. gordonae, and minimum inhibitory concentration values were also determined using the standard antituberculotic drug isoniazid (INH) as a reference. Structure-activity relationships were also studied. The mode of action of the test compounds was investigated using transmission electron microscopy, high-performance liquid chromatography, and matrix-assisted desorption/ionization mass spectrometry. Several test substances proved to be as potent as INH, but their antimycobacterial spectra were broader than that of INH. Our findings suggest that their mode of action is probably through the inhibition of mycobacterial cell wall biosynthesis.}, year = {2017}, eissn = {1521-4184}, orcid-numbers = {Márk, László/0000-0002-9301-8159} } @article{MTMT:3157933, title = {Synthesis of carotenoid-monosaccharide conjugates via azide–alkyne click-reaction}, url = {https://m2.mtmt.hu/api/publication/3157933}, author = {Agócs, Attila and Bokor, Éva and Takátsy, Anikó and Lóránd, Tamás and Deli, József and Somsák, László and Nagy, Veronika}, doi = {10.1016/j.tet.2016.12.035}, journal-iso = {TETRAHEDRON}, journal = {TETRAHEDRON}, volume = {73}, unique-id = {3157933}, issn = {0040-4020}, year = {2017}, eissn = {1464-5416}, pages = {519-526}, orcid-numbers = {Deli, József/0000-0002-0625-6117; Somsák, László/0000-0002-9103-9845; Nagy, Veronika/0000-0002-9019-7980} }