Biological and chemical insight into Gaultheria procumbens fruits: a rich source of anti-inflammatory and antioxidant salicylate glycosides and procyanidins for food and functional application

Food Funct. 2020 Sep 23;11(9):7532-7544. doi: 10.1039/d0fo01750g.


The fruits of Gaultheria procumbens are traditionally used for culinary and healing purposes as anti-inflammatory agents. In the present work, the active components of the fruits were identified (UHPLC-PDA-ESI-MS3, preparative HPLC isolation, and NMR structural studies), and their biological capacity was evaluated in vitro in cell-based and non-cellular models. The fruits were revealed to be the richest known dietary source of salicylates (38.5 mg per g fruit dw). They are also rich in procyanidins (28.5 mg per g fruit dw). Among five tested solvents, acetone was the most efficient in concentrating the phenolic matrix (39 identified compounds; 191.3 mg g-1, 121.7 mg g-1, and 50.9 mg g-1 dry extract for total phenolics, salicylates, and procyanidins, respectively). In comparison to positive controls (dexamethasone, indomethacin, and quercetin), the extract (AE) and pure salicylates exhibited strong inhibitory activity towards pro-inflammatory enzymes (cyclooxygenase-2 and hyaluronidase). The analytes were found to be non-cytotoxic (flow cytometry) towards human neutrophils ex vivo. Moreover, they significantly, in a dose-dependent manner, downregulated the release of ROS, TNF-α, IL-1β, and elastase-2 and slightly inhibited the secretion of IL-8 and metalloproteinase-9 in the cells. The observed effects might support the usage of G. procumbens fruits as functional components of an anti-inflammatory diet and indicate the potential of AE for use in adjuvant treatment of inflammatory disorders cross-linked with oxidative stress and associated with the excessive production of TNF-α, IL-1β, and elastase-2.

MeSH terms

  • Anti-Inflammatory Agents / chemistry*
  • Anti-Inflammatory Agents / pharmacology
  • Antioxidants / chemistry*
  • Antioxidants / pharmacology
  • Biflavonoids / chemistry*
  • Biflavonoids / pharmacology
  • Catechin / chemistry*
  • Catechin / pharmacology
  • Fruit / chemistry
  • Gaultheria / chemistry*
  • Glycosides / chemistry*
  • Glycosides / pharmacology
  • Humans
  • Interleukin-8 / immunology
  • Neutrophils / drug effects
  • Neutrophils / immunology
  • Plant Extracts / chemistry*
  • Plant Extracts / pharmacology
  • Proanthocyanidins / chemistry*
  • Proanthocyanidins / pharmacology


  • Anti-Inflammatory Agents
  • Antioxidants
  • Biflavonoids
  • Glycosides
  • Interleukin-8
  • Plant Extracts
  • Proanthocyanidins
  • procyanidin
  • Catechin