THE MECHANISM OF ACTION OF ANTROQUINONOL

Antroquinonol binds directly to isoprenyltransferase (farnesyltransferase, FTase and geranylgeranyltransferase-I, GGTase-1) and inhibits their enzyme activities which involve in the activation of Ras superfamily proteins in cancer cells, resulting in interference with the Ras/Rho-PI3K-Akt-mTOR pathway, leading to the activation of apoptosis and autophagy.

With this unique mechanism of action, Antroquinonol has so far gained orphan drug designations in treating pancreatic cancer, acute myeloid leukemia (AML) and hepatocellular carcinomas (HCCs).

View research publications on Antroquinonol in Oncology.

For more clinical trial information please visit ClinicalTrials.gov.

Reference:

  1. Lin, Hsien-Chun, et al. “Antroquinonol, a ubiquinone derivative from the mushroom Antrodia camphorata, inhibits colon cancer stem cell-like properties: insights into the molecular mechanism and inhibitory targets.” Journal of agricultural and food chemistry 65.1 (2016): 51-59.
  2. Lee, Wai-Theng, et al. “Antroquinonol from Antrodia Camphorata suppresses breast tumor migration/invasion through inhibiting ERK-AP-1-and AKT-NF-κB-dependent MMP-9 and epithelial-mesenchymal transition expressions.” Food and chemical toxicology 78 (2015): 33-41.
  3. Thiyagarajan, Varadharajan, May-Jywan Tsai, and Ching-Feng Weng. “Antroquinonol targets FAK-signaling pathway suppressed cell migration, invasion, and tumor growth of C6 glioma.” PLoS One 10.10 (2015): e0141285.
  4. Ho, Ching-Liang, et al. “Antroquinonol blocks Ras and Rho signaling via the inhibition of protein isoprenyltransferase activity in cancer cells.” Biomedicine & Pharmacotherapy 68.8 (2014): 1007-1014.Antroquinonol inhibits NSCLC proliferation by altering PI3K/mTOR proteins and miRNA expression profiles. Mutation Research; 707:42-52.        
  5. Yu, Chia-Chun, et al. “Antroquinonol, a natural ubiquinone derivative, induces a cross talk between apoptosis, autophagy and senescence in human pancreatic carcinoma cells.” The Journal of nutritional biochemistry 23.8 (2012): 900-907.      
  6. Chiang, Po-Cheng, et al. “Antroquinonol displays anticancer potential against human hepatocellular carcinoma cells: a crucial role of AMPK and mTOR pathways.” Biochemical pharmacology 79.2 (2010): 162-171.