2. Academic Validation
  3. Potent anti-cancer effect of 3'-hydroxypterostilbene in human colon xenograft tumors

Potent anti-cancer effect of 3'-hydroxypterostilbene in human colon xenograft tumors

  • PLoS One. 2014 Nov 12;9(11):e111814. doi: 10.1371/journal.pone.0111814.
Tzu-Chun Cheng 1,  Ching-Shu Lai 2,  Min-Ching Chung 2,  Nagabhushanam Kalyanam 3,  Muhammed Majeed 3,  Chi-Tang Ho 4,  Yuan-Soon Ho 5,  Min-Hsiung Pan 6
Affiliations

Affiliations

  • 1 Graduate Institute of Medical Sciences, College of Medicine, Taipei Medical University, Taipei, Taiwan.
  • 2 Institute of Food Science and Technology, National Taiwan University, Taipei, Taiwan.
  • 3 Sabinsa Corporation, East Windsor, New Jersey, United States of America.
  • 4 Department of Food Science, Rutgers University, New Brunswick, New Jersey, United States of America.
  • 5 Graduate Institute of Medical Sciences, College of Medicine, Taipei Medical University, Taipei, Taiwan; Department of Laboratory Medicine, Taipei Medical University Hospital, Taipei, Taiwan; School of Medical Laboratory Science and Biotechnology, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan; Comprehensive Cancer Center, Taipei Medical University, Taipei, Taiwan.
  • 6 Institute of Food Science and Technology, National Taiwan University, Taipei, Taiwan; Department of Medical Research, China Medical University Hospital, China Medical University, Taichung, Taiwan.
PMID: 25389774 DOI: 10.1371/journal.pone.0111814
Abstract

Here we report that 3'-hydroxypterostilbene (HPSB), a natural pterostilbene analogue, was more potent than pterostilbene against the growth of human Cancer cells (COLO 205, HCT-116, and HT-29) with measured IC50 values of 9.0, 40.2, and 70.9 µM, respectively. We found that HPSB effectively inhibited the growth of human colon Cancer cells by inducing Apoptosis and Autophagy. Autophagy occurred at an early stage and was observed through the formation of acidic vesicular organelles and microtubule-associated protein 1 LIGHT chain 3-II production. At the molecular levels, the results from western blot analysis showed that HPSB significantly down-regulated phosphatidylinositol 3-kinase (PI3K)/Akt and mitogen-activated protein kinases (MAPKs) signalings including decreased the phosphorylation of mammalian target of rapamycin (mTOR). Significant therapeutic effects were demonstrated in vivo by treating nude mice bearing COLO 205 tumor xenografts with HPSB (10 mg/kg i.p.). These inhibitory effects were accompanied by mechanistic down-regulation of the protein levels of cyclooxygenase-2 (COX-2), matrix metallopeptidase-9 (MMP-9), vascular endothelial growth factor (VEGF), and cyclin D1, as well as by the induction of Apoptosis in colon tumors. Our findings suggest that HPSB could serve as a novel promising agent for colon Cancer treatment.

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