title: Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro.
abstract: Cudraflavone B (1) is a prenylated flavonoid found in large amounts in the roots of Morus alba, a plant used as a herbal remedy for its reputed anti-inflammatory properties. The present study shows that this compound causes a significant inhibition of inflammatory mediators in selected in vitro models. Thus, 1 was identified as a potent inhibitor of tumor necrosis factor α (TNFα) gene expression and secretion by blocking the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages derived from a THP-1 human monocyte cell line. The NF-κB activity reduction resulted in the inhibition of cyclooxygenase 2 (COX-2) gene expression. Compound 1 acts as a COX-2 and COX-1 inhibitor with higher selectivity toward COX-2 than indomethacin. Pretreatment of cells by 1 shifted the peak in an regulatory gene zinc-finger protein 36 (ZFP36) expression assay. This natural product has noticeable anti-inflammatory properties, suggesting that 1 potentially could be used for development as a nonsteroidal anti-inflammatory drug lead.
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého 1-3, Brno, 612 42, Czech Republic. hosekj@vfu.cz
authors.forename: Jan
authors.initials: J
authors.lastname: Hošek
authors.forename: Milan
authors.initials: M
authors.lastname: Bartos
authors.forename: Stanislav
authors.initials: S
authors.lastname: Chudík
authors.forename: Stefano
authors.initials: S
authors.lastname: Dall'Acqua
authors.forename: Gabbriella
authors.initials: G
authors.lastname: Innocenti
authors.forename: Murat
authors.initials: M
authors.lastname: Kartal
authors.forename: Ladislav
authors.initials: L
authors.lastname: Kokoška
authors.forename: Peter
authors.initials: P
authors.lastname: Kollár
authors.forename: Zsófia
authors.initials: Z
authors.lastname: Kutil
authors.forename: Přemysl
authors.initials: P
authors.lastname: Landa
authors.forename: Radek
authors.initials: R
authors.lastname: Marek
authors.forename: Veronika
authors.initials: V
authors.lastname: Závalová
authors.forename: Milan
authors.initials: M
authors.lastname: Žemlička
authors.forename: Karel
authors.initials: K
authors.lastname: Šmejkal
mesh_terms: D000199:Actins / Q000187:drug effects; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D051545:Cyclooxygenase 1 / Q000187:drug effects; D052246:Cyclooxygenase 2 Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D008264:Macrophages / Q000187:drug effects; D015394:Molecular Structure; D031625:Morus / Q000737:chemistry*; D016328:NF-kappa B / Q000037:antagonists & inhibitors*; D018517:Plant Roots / Q000737:chemistry; D051816:Tristetraprolin / Q000187:drug effects / Q000235:genetics; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors* / Q000235:genetics
chemical_list: D000199:Actins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D005419:Flavonoids; D016328:NF-kappa B; D051816:Tristetraprolin; D014409:Tumor Necrosis Factor-alpha; C497552:ZFP36 protein, human; C542041:cudraflavone B; D051545:Cyclooxygenase 1; C496511:PTGS1 protein, human