Inhibition of host- and bacteria-derived proteinases by natural anthocyanins

J Periodontal Res. 2011 Oct;46(5):550-7. doi: 10.1111/j.1600-0765.2011.01372.x. Epub 2011 Apr 21.

Abstract

Background and objectives: Host- and bacteria-derived proteinases are considered to play critical roles in periodontitis progression. This study investigated the ability of a blackcurrant extract and its major anthocyanins (cyanidin-3-O-glucoside, cyanidin-3-O-rutinoside and delphinidin-3-O-rutinoside) to inhibit the activity of matrix metalloproteinases (MMPs), neutrophil elastase and periodontopathogen (Porphyromonas gingivalis, Tannerella forsythia and Treponema denticola) proteinases.

Material and methods: Enzyme inhibition was detected using fluorometric and colorimetric assays after incubating blackcurrant extract and its major anthocyanins (at concentrations of 6.25, 12.5, 25 and 50 μg/mL) with MMPs, elastase or bacterial proteinases, along with their specific substrates. Substrate degradation was recorded every hour for up to 4 h.

Results: The blackcurrant extract (50 μg/mL) inhibited all proteinases tested. MMP-1 and MMP-9 were significantly inhibited by pure anthocyanins at concentrations ranging from 6.25 to 50 μg/mL. Elastase activity was inhibited by cyanidin-3-O-glucoside and cyanidin-3-O-rutinoside in the range of 6.25-50 μg/mL and by delphinidin-3-O-rutinoside at 50 μg/mL. P. gingivalis, T. forsythia and T. denticola proteinases were also significantly inhibited by pure anthocyanins. In all cases, enzyme inhibition was time-dependent.

Conclusion: Our study showed that a blackcurrant extract and its major anthocyanins were able to inhibit the activity of host- and bacteria-derived proteinases. This suggests that such natural compounds may represent promising agents for use in adjunctive treatments for periodontitis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anthocyanins / pharmacology*
  • Bacterial Proteins / antagonists & inhibitors
  • Bacteroides / enzymology
  • Glucosides / pharmacology
  • Humans
  • Leukocyte Elastase / adverse effects
  • Matrix Metalloproteinase 1 / adverse effects
  • Matrix Metalloproteinase Inhibitors
  • Plant Extracts / pharmacology*
  • Porphyromonas gingivalis / enzymology
  • Protease Inhibitors / pharmacology*
  • Proteolysis
  • Ribes / chemistry*
  • Treponema denticola / enzymology

Substances

  • Anthocyanins
  • Bacterial Proteins
  • Glucosides
  • Matrix Metalloproteinase Inhibitors
  • Plant Extracts
  • Protease Inhibitors
  • cyanidin-3-O-beta-glucopyranoside
  • delphinidin-3-rutinoside
  • Leukocyte Elastase
  • Matrix Metalloproteinase 1
  • cyanidin 3-rutinoside