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Inhibition of In Vitro Leukotriene B-4 Biosynthesis in Human Neutrophil Granulocytes and Docking Studies of Natural Quinones
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SYSNO ASEP 0395042 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Inhibition of In Vitro Leukotriene B-4 Biosynthesis in Human Neutrophil Granulocytes and Docking Studies of Natural Quinones Author(s) Landa, Přemysl (UEB-Q) RID, ORCID
Kutil, Zsófia (UEB-Q)
Temml, V. (AT)
Malík, J. (CZ)
Kokoška, L. (CZ)
Widowitz, U. (AT)
Přibylová, Marie (UEB-Q)
Dvořáková, Marcela (UEB-Q) RID, ORCID
Maršík, Petr (UEB-Q) RID, ORCID
Schuster, D. (AT)
Bauer, R. (AT)
Vaněk, Tomáš (UEB-Q) RID, ORCIDSource Title Natural Product Communications - ISSN 1934-578X
Roč. 8, č. 1 (2013), s. 105-108Number of pages 4 s. Language eng - English Country US - United States Keywords 5-Lipoxygenase ; Anti-inflammatory activity ; Dual COX/LOX inhibition Subject RIV GM - Food Processing R&D Projects GP525/09/P528 GA ČR - Czech Science Foundation (CSF) MEB061112 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z50380511 - UEB-Q (2005-2011) UT WOS 000314617200027 Annotation Quinones are compounds frequently contained in medicinal plants used for the treatment of inflammatory diseases. Therefore, the impact of plant-derived quinones on the arachidonic acid metabolic pathway is worthy of investigation. In this study, twenty-three quinone compounds of plant origin were tested in vitro for their potential to inhibit leukotriene B-4 (LTB4) biosynthesis in activated human neutrophil granulocytes with 5-lipoxygenase (5-LOX) activity. The benzoquinones primin (3) and thymohydroquinone (4) (IC50 = 4.0 and 4.1 mu M, respectively) showed activity comparable with the reference inhibitor zileuton (IC50 = 4.1 mu M). Moderate activity was observed for the benzoquinone thymoquinone (2) (IC50 = 18.2 mu M) and the naphthoquinone shikonin (1) (IC50 = 24.3 mu M). The anthraquinone emodin and the naphthoquinone plumbagin (5) displayed only weak activities (IC50 > 50 mu M). The binding modes of the active compounds were further evaluated in silico by molecular docking to the human 5-LOX crystal structure. This process supports the biological data and suggested that, although the redox potential is responsible for the quinone's activity on multiple targets, in the case of 5-LOX the molecular structure plays a vital role in the inhibition. The obtained results suggest primin as a promising compound for the development of dual COX-2/5-LOX inhibitors. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2014
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