Dietary polyphenol oleuropein and its metabolite hydroxytyrosol are moderate skin permeable elastase and collagenase inhibitors with synergistic cellular antioxidant effects in human skin fibroblasts

Int J Food Sci Nutr. 2022 Jun;73(4):460-470. doi: 10.1080/09637486.2021.1996542. Epub 2021 Oct 31.

Abstract

Oleuropein (OLE) and hydroxytyrosol (HT) are dietary polyphenols with skin beneficial effects but their effects on skin-ageing-related enzymes are not clear. Herein, we evaluated their inhibitory effects on elastase and collagenase. OLE and HT (62.5-1 000 μM) showed moderate anti-elastase and anti-collagenase effects (5.1-26.3%, 5.8-12.2% and 12.6-31.0%, 11.6-31.9% inhibition, respectively). Combinations of OLE and HT (1:1 ratio) exerted synergistic inhibitory effects on elastase, which were supported by their combination index (CI), kinetic assay and computational docking. Moreover, HT (100 μM) reduced hydrogen peroxide (H2O2)-induced cytotoxicity and reactive oxygen species (ROS) in human dermal fibroblast cells by 21.8 and 15.2%, respectively. In addition, combinations of OLE and HT (6.25/6.25-100/100 μM) exerted synergistic cytoprotective effects by reducing ROS levels by 7.6-37.3% with CIs of 0.17-0.44, respectively. The findings from this study support the cosmeceutical activities of OLE and HT but further research is warranted to evaluate their anti-skin-ageing effects using in vivo models.

Keywords: Oleuropein; collagenase; elastase; hydroxytyrosol; skin protection.

MeSH terms

  • Antioxidants* / pharmacology
  • Fibroblasts
  • Humans
  • Hydrogen Peroxide
  • Iridoid Glucosides
  • Iridoids / pharmacology
  • Matrix Metalloproteinase Inhibitors
  • Pancreatic Elastase
  • Phenylethyl Alcohol / analogs & derivatives
  • Polyphenols* / pharmacology
  • Reactive Oxygen Species

Substances

  • Antioxidants
  • Iridoid Glucosides
  • Iridoids
  • Matrix Metalloproteinase Inhibitors
  • Polyphenols
  • Reactive Oxygen Species
  • 3,4-dihydroxyphenylethanol
  • oleuropein
  • Hydrogen Peroxide
  • Pancreatic Elastase
  • Phenylethyl Alcohol