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Natural Compound Cudraflavone B Shows Promising Anti-inflammatory Properties in Vitro

2011; American Chemical Society; Volume: 74; Issue: 4 Linguagem: Inglês

10.1021/np100638h

1520-6025

Jan Hošek, Milan Bartoš, Stanislav Chudík, Stefano Dall’Acqua, Gabbriella Innocenti, Murat Kartal, Ladislav Kokoška, Péter Kollár, Zsófia Kutil, Přemysl Landa, Radek Marek, Veronika Müller Závalová, Milan Žemlička, Karel Šmejkal,

NF-κB Signaling Pathways

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.