Modulatory Effect of Diosmin and Diosmetin on Metalloproteinase Activity and Inflammatory Mediators in Human Skin Fibroblasts Treated with Lipopolysaccharide

Molecules. 2022 Jul 1;27(13):4264. doi: 10.3390/molecules27134264.

Abstract

Diosmin is widely used as a venoactive drug in the pharmacological treatment of chronic venous disorders. It exerts a strong protective effect on blood vessels via an increase in the elasticity of vessel walls and reduces the permeability of capillary walls, thereby producing an anti-edematous effect. In this paper, we investigated the effectiveness of diosmin and diosmetin in modulating the level of proinflammatory factors in human skin fibroblasts treated with lipopolysaccharide (LPS). Two variants of the experiments were performed: the flavonoid was added 2 h prior to or 24 h after LPS stimulation. Our study revealed that both flavonoids reduced the levels of IL-6 and Il-1β as well as COX-2 and PGE2 but had no impact on IL-10. However, the addition of the compounds prior to the LPS addition was more effective. Moreover, diosmetin modulated the proinflammatory factors more strongly than diosmin. Our investigations also showed that both flavonoids were potent inhibitors of elastase and collagenase activity, and no differences between the glycoside and aglycone forms were observed.

Keywords: anti-inflammatory activity; chronic venous disorders; diosmetin; diosmin; lipopolysaccharide; metalloproteinase.

MeSH terms

  • Diosmin* / pharmacology
  • Fibroblasts
  • Flavonoids / pharmacology
  • Humans
  • Inflammation Mediators
  • Lipopolysaccharides / pharmacology
  • Metalloproteases

Substances

  • Flavonoids
  • Inflammation Mediators
  • Lipopolysaccharides
  • Diosmin
  • Metalloproteases
  • diosmetin

Grants and funding

This research received no external funding.