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oleocanthal (Hyeda)

phenolic compound in extra virgin olive oil in amounts up to 200 ug/mL [4] Indications: - transdermal olive oil formulation for relief of inflammation [2] Adverse effects: - responsible for the burning sensation that occurs in the back of the throat when consuming extra virgin olive oil Mechanism of action: - in vitro activity of 10-20 uM oleocanthal - inhibits COX1 & COX2 - 9-10 mg of oleocanthal contains 10% of anti-inflammatory activity of 200-400 mg of ibuprofen [4] - amount in 50 g (4 tbsp) of extra virgin olive oil - inhibits cell proliferation, cell migration, & invasion of breast cancer & prostate cancer cells via inhibition of c-Met - inhibits AMPK in colon cancer cells - inhibits macrophage inflammatory protein-1-alpha in multiple myeloma - induces cell death of cancer cells in vitro - induces both necrosis & apoptosis of cancer cells in vitro via induction of lysosomal membrane permeabilization - cancer cells have fragile lysosomal membranes compared to non-cancerous cells - in the absence of serum, oleocanthal induces necrosis of cancer cells (does not induce cleavage of caspase-3) - suppresses proliferation of non-cancer cells by inhibiting Rb protein phosphorylation at Ser608 - normal cells resume proliferation 72 hours after oleocanthal treatment - induces a reversible cell cycle arrest in non-cancerous cells that retain their viability - inhibits acid sphingomyelinase which destabilizes the lysosomal membrane - cancer cells overcome lysosomal membrane fragility by overexpression of HSP70 which enhances acid sphingomyelinase activity

Interactions

drug interactions drug adverse effects of NSAIDs monitor with non steroidal anti-inflammatory agents (NSIADs)

General

aldehyde alkene; olefin ester non-steroidal anti-inflammatory agent (NSAID) phenol

Properties

INHIBITS: cyclooxygenase

Database Correlations

PUBCHEM correlations

References

  1. LeGendre O, Breslin PA, Foster DA (-)-Oleocanthal rapidly and selectively induces cancer cell death via lysosomal membrane permeabilization (LMP). Molecular & Cellular Oncology. 23 Jan 2015. http://dx.doi.org/10.1080/23723556.2015.1006077
  2. PubChem: 16681728
  3. Wikipedia: Oleocanthal http://en.wikipedia.org/wiki/Oleocanthal
  4. Beauchamp GK, Keast RSJ, Morel D et al Phytochemistry: Ibuprofen-like activity in extra-virgin olive oil. Nature 437, 45-46 (1 September 2005) http://www.nature.com/nature/journal/v437/n7055/full/437045a.html
  5. Akl MR, Ayoub NM, Mohyeldin MM et al Olive phenolics as c-Met inhibitors: (-)-Oleocanthal attenuates cell proliferation, invasiveness, and tumor growth in breast cancer models. PLoS One. 2014 May 21;9(5):e97622 PMID: 24849787