Bioavailable Citrus sinensis Extract: polyphenolic composition and biological activity: Polyphenolic Composition and Biological Activity

Giacomo Pepe, Francesco Pagano, Simona Adesso, Eduardo Sommella, Carmine Ostacolo, Michele Manfra, Marcello Chieppa, Marina Sala, Mariateresa Russo, Stefania Marzocco, Pietro Campiglia

Research output: Contribution to journalArticlepeer-review


Citrus plants contain large amounts of flavonoids with beneficial effects on human health. In the present study, the antioxidant and anti-inflammatory potential of bioavailable polyphenols from Citrus sinensis was evaluated in vitro and ex vivo, using the murine macrophages cell line J774A.1 and primary peritoneal macrophages. Following simulated gastro-intestinal digestion, the in vitro bioavailability of Citrus sinensis polyphenolic extract was assessed using the human cell line Caco-2 grown as monolayers on a transwell membrane. Data demonstrated a relative permeation of its compounds (8.3%). Thus, the antioxidant and anti-inflammatory effect of polyphenolic Citrus sinensis fraction (Cs) was compared to the bioavailable one (CsB). Results revealed that Citrus extract were able to reduce macrophages pro-inflammatory mediators, including nitric oxide, iNOS, COX-2 and different cytokines. Moreover, the effect of Citrus sinensis polyphenols was associated with antioxidant effects, such as a reduction of reactive oxygen species (ROS) and heme-oxygenase-1 (HO-1) increased expression. Our results provide evidence that the bioavailable polyphenolic constituents of the Citrussinensis extract accumulate prevalently at intestinal level and could reach systemic circulation exerting their effect. The bioavailable fraction showed a higher anti-inflammatory and antioxidant potential compared to the initial extract, thus highlighting its potential nutraceutical value.

Original languageEnglish
Pages (from-to)1-15
Number of pages15
Issue number4
Publication statusPublished - Apr 15 2017


  • Animals
  • Anti-Inflammatory Agents
  • Antioxidants
  • Cell Survival
  • Citrus sinensis
  • Cyclooxygenase 2
  • Cytokines
  • Flavonoids
  • Fruit and Vegetable Juices
  • Gastrointestinal Absorption
  • Heme Oxygenase-1
  • Humans
  • Inflammation Mediators
  • Lipopolysaccharides
  • Macrophages, Peritoneal
  • Mice
  • Nitric Oxide Synthase Type II
  • Phytochemicals
  • Plant Extracts
  • Polyphenols
  • Protein Transport
  • Reactive Oxygen Species
  • Spectrum Analysis
  • Transcription Factor RelA
  • Journal Article


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