Anti-osteoclastic effects of C-glucosidic ellagitannins mediated by actin perturbation

Eur J Cell Biol. 2018 Nov;97(8):533-545. doi: 10.1016/j.ejcb.2018.09.003. Epub 2018 Sep 24.


Actin subunits assemble into actin filaments whose dynamics and three-dimensional architectures are further regulated by a variety of cellular factors to establish the functional actin cytoskeleton. The C-glucosidic ellagitannin vescalagin and its simpler analogue vescalin, affect both the dynamics and the ultrastructure of the actin cytoskeleton by directly binding to F-actin. Herein, we show that in vitro, the two compounds induce the formation of distinct F-actin networks characterized by different superstructures and dynamics. In living mature osteoclasts, highly specialized bone-degrading cells that constantly remodel their cytoskeleton, vescalagin and vescalin alter actin dynamics at podosomes and compromise the integrity of the podosome belt that forms the bone-degrading apparatus. Both compounds target the bone-resorbing activity at concentrations that preserve osteoclastic maturation and survival and with no detectable impact on the behaviour of bone-forming osteoblastic cells. This anti-osteoclastic activity of vescalagin and vescalin reveals the potential of targeting actin dynamics as a new therapeutic opportunity and, in this case, as a plausible approach for the local treatment of osteoporosis.

Keywords: Actin dynamics; Cytoskeleton; Medicinal biology; Osteoclast biology; Podosomes; Polyphenol sciences.

MeSH terms

  • Actin Cytoskeleton / metabolism
  • Actins / metabolism*
  • Animals
  • Bone Resorption / pathology
  • Cell Adhesion / drug effects
  • Cell Differentiation
  • Cell Survival / drug effects
  • Cytoskeleton / metabolism
  • Extracellular Matrix / metabolism
  • Glucosides / chemistry
  • Glucosides / pharmacology*
  • Hydrolyzable Tannins / chemistry
  • Hydrolyzable Tannins / pharmacology*
  • Mice, Inbred C57BL
  • Osteoclasts / cytology*
  • Osteoclasts / drug effects
  • Osteoclasts / metabolism*
  • Podosomes / metabolism
  • Polymerization


  • Actins
  • Glucosides
  • Hydrolyzable Tannins
  • ellagitannin
  • vescalagin