Potential Therapeutic Anti-Inflammatory and Immunomodulatory Effects of Dihydroflavones, Flavones, and Flavonols

Molecules. 2020 Feb 24;25(4):1017. doi: 10.3390/molecules25041017.

Abstract

Systemic inflammation, circulating immune cell activation, and endothelial cell damage play a critical role in vascular pathogenesis. Flavonoids have shown anti-inflammatory effects. In this study, we investigated the effects of different flavonoids on the production of pro-inflammatory interleukin (IL) 1β, 6, and 8, and tumor necrosis factor α (TNF-α), in peripheral blood cells. Methods: We studied the whole blood from 36 healthy donors. Lipopolysaccharide (LPS)-stimulated (0.5 μg/mL) whole-blood aliquots were incubated in the presence or absence of different concentrations of quercetin, rutin, naringenin, naringin, diosmetin, and diosmin for 6 h. Cultures were centrifuged and the supernatant was collected in order to measure IL-1β, TNF-α, IL-6, and IL-8 production using specific immunoassay techniques. This production was significantly inhibited by quercetin, naringenin, naringin, and diosmetin, but in no case by rutin or diosmin. Flavonoids exert different effects, maybe due to the differences between aglycons and glucosides present in their chemical structures. However, these studies suggest that quercetin, naringenin, naringin, and diosmetin could have a potential therapeutic effect in the inflammatory process of cardiovascular disease.

Keywords: IL-1β; IL-6; IL-8; TNF-α; aglycons; flavonoids; glycosides; pro-inflammatory cytokines.

MeSH terms

  • Anti-Inflammatory Agents / pharmacology*
  • Diosmin / pharmacology
  • Dose-Response Relationship, Immunologic
  • Female
  • Flavanones / pharmacology*
  • Flavones / pharmacology*
  • Flavonoids / pharmacology*
  • Flavonols / pharmacology*
  • Healthy Volunteers
  • Humans
  • Interleukin-1beta / biosynthesis
  • Interleukin-1beta / immunology
  • Interleukin-6 / biosynthesis
  • Interleukin-6 / immunology
  • Interleukin-8 / biosynthesis
  • Interleukin-8 / immunology
  • Leukocytes, Mononuclear / cytology
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / immunology
  • Lipopolysaccharides / antagonists & inhibitors
  • Lipopolysaccharides / pharmacology
  • Male
  • Primary Cell Culture
  • Quercetin / pharmacology*
  • Rutin / pharmacology
  • Tumor Necrosis Factor-alpha / biosynthesis
  • Tumor Necrosis Factor-alpha / immunology
  • Young Adult

Substances

  • Anti-Inflammatory Agents
  • Flavanones
  • Flavones
  • Flavonoids
  • Flavonols
  • IL1B protein, human
  • IL6 protein, human
  • Interleukin-1beta
  • Interleukin-6
  • Interleukin-8
  • Lipopolysaccharides
  • Tumor Necrosis Factor-alpha
  • Rutin
  • Diosmin
  • Quercetin
  • naringenin
  • naringin
  • diosmetin