| Summary: | Noni (<i>Morinda citrifolia</i> L.) fruit juice has been used in Polynesia as a traditional folk medicine and is very popular worldwide as a functional food supplement. In this study, compounds present in Hawaiian Noni fruit juice, with anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells were identified. Five compounds were isolated using a bioassay-driven technique and phytochemical analysis of noni fruit juice: asperulosidic acid (<b>1</b>), rutin (<b>2</b>), nonioside A (<b>3</b>), (2<i>E</i>,4<i>E</i>,7<i>Z</i>)-deca-2,4,7-trienoate-2-<i>O</i>-β-<span style="font-variant: small-caps;">d</span>-glucopyranosyl-β-<span style="font-variant: small-caps;">d</span>-glucopyranoside (<b>4</b>), and tricetin (<b>5</b>). The structures of these five compounds were determined via NMR spectroscopy and LC/MS. In an anti-inflammatory assay, compounds <b>1</b>–<b>5</b> inhibited the production of nitric oxide (NO), which is a proinflammatory mediator, in LPS-stimulated macrophages. Moreover, the mechanisms underlying the anti-inflammatory effects of compounds <b>1</b>–<b>5</b> were investigated. Parallel to the inhibition of NO production, treatment with compounds <b>1</b>–<b>5</b> downregulated the expression of IKKα/β, I-κBα, and NF-κB p65 in LPS-stimulated macrophages. Furthermore, treatment with compounds <b>1</b>–<b>5</b> downregulated the expression of nitric oxide synthase and cyclooxygenase-2. Thus, these data demonstrated that compounds <b>1</b>–<b>5</b> present in noni fruit juice, exhibited potential anti-inflammatory activity; these active compounds may contribute preventively and therapeutically against inflammatory diseases.
|
|---|
