Anti-Inflammatory and Proliferative Properties of Luteolin-7-O-Glucoside

Int J Mol Sci. 2021 Jan 28;22(3):1321. doi: 10.3390/ijms22031321.

Abstract

Flavonoids display a broad range of structures and are responsible for the major organoleptic characteristics of plant-derived foods and beverages. Recent data showed their activity, and in particular of luteolin-7-O-glucoside (LUT-7G), in reduction of oxidative stress and inflammatory mechanisms in different physiological systems. In this paper, we tried to elucidate how LUT-7G could exert both antioxidant and anti-inflammatory effects in endothelial cells cultured in vitro. Here, we showed that LUT-7G is able to inhibit the STAT3 pathway, to have an antiproliferative action, and an important antioxidant property in HUVEC cells. These properties are exerted by the flavone in endothelial through the transcriptional repression of a number of inflammatory cytokines and their receptors, and by the inhibition of ROS generation. ROS and STAT3 activation has been correlated with the production of oxysterols and other hydroxylated fatty acids, and they have been recognized important as players of atherogenesis and cardiocirculatory system diseases. The analysis of the general production pathway of these hydroxylated species, showed a strong decrease of cholesterol hydroxylated species such as 7-alpha-hydroxicholesterol, 7-beta-hydroxicholesterol by the treatment with LUT-7G. This confirms the anti-inflammatory properties of LUT-7G also in the endothelial district, showing for the first time the molecular pathway that verify previous postulated cardiovascular benefits of this flavone.

Keywords: STAT3; flavonoids; hydroxylation; inflammation; luteolin-7-O-glucoside.

MeSH terms

  • Anti-Inflammatory Agents / pharmacology*
  • Antioxidants / pharmacology*
  • Cell Line
  • Cell Proliferation
  • Endothelial Cells / chemistry
  • Endothelial Cells / cytology
  • Endothelial Cells / drug effects
  • Fatty Acids / metabolism
  • Flavones / pharmacology*
  • Glucosides / pharmacology*
  • Human Umbilical Vein Endothelial Cells
  • Humans
  • Hydroxylation
  • Keratinocytes / chemistry
  • Keratinocytes / cytology*
  • Keratinocytes / drug effects
  • Metabolomics
  • Oxysterols / metabolism
  • Reactive Oxygen Species / metabolism
  • Sialyltransferases / metabolism*
  • Signal Transduction / drug effects

Substances

  • Anti-Inflammatory Agents
  • Antioxidants
  • Fatty Acids
  • Flavones
  • Glucosides
  • Oxysterols
  • Reactive Oxygen Species
  • luteolin-7-glucoside
  • Sialyltransferases
  • ST3GAL4 protein, human