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Antitumor efficacy of piperine in the treatment of human HER2-overexpressing breast cancer cells.

Abstract
Piperine is a bioactive component of black pepper, Piper nigrum Linn, commonly used for daily consumption and in traditional medicine. Here, the molecular mechanisms by which piperine exerts antitumor effects in HER2-overexpressing breast cancer cells was investigated. The results showed that piperine strongly inhibited proliferation and induced apoptosis through caspase-3 activation and PARP cleavage. Furthermore, piperine inhibited HER2 gene expression at the transcriptional level. Blockade of ERK1/2 signaling by piperine significantly reduced SREBP-1 and FAS expression. Piperine strongly suppressed EGF-induced MMP-9 expression through inhibition of AP-1 and NF-κB activation by interfering with ERK1/2, p38 MAPK, and Akt signaling pathways resulting in a reduction in migration. Finally, piperine pretreatment enhanced sensitization to paclitaxel killing in HER2-overexpressing breast cancer cells. Our findings suggest that piperine may be a potential agent for the prevention and treatment of human breast cancer with HER2 overexpression.
AuthorsMinh Truong Do, Hyung Gyun Kim, Jae Ho Choi, Tilak Khanal, Bong Hwan Park, Thu Phuong Tran, Tae Cheon Jeong, Hye Gwang Jeong
JournalFood chemistry (Food Chem) Vol. 141 Issue 3 Pg. 2591-9 (Dec 01 2013) ISSN: 1873-7072 [Electronic] England
PMID23870999 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2013 Elsevier Ltd. All rights reserved.
Chemical References
  • Alkaloids
  • Antineoplastic Agents, Phytogenic
  • Benzodioxoles
  • Piperidines
  • Plant Extracts
  • Polyunsaturated Alkamides
  • ERBB2 protein, human
  • Receptor, ErbB-2
  • p38 Mitogen-Activated Protein Kinases
  • Caspase 3
  • piperine
Topics
  • Alkaloids (pharmacology)
  • Antineoplastic Agents, Phytogenic (pharmacology)
  • Apoptosis (drug effects)
  • Benzodioxoles (pharmacology)
  • Breast Neoplasms (drug therapy, genetics, metabolism, physiopathology)
  • Caspase 3 (genetics, metabolism)
  • Female
  • Gene Expression Regulation, Neoplastic (drug effects)
  • Humans
  • Piperidines (pharmacology)
  • Plant Extracts (pharmacology)
  • Polyunsaturated Alkamides (pharmacology)
  • Receptor, ErbB-2 (genetics, metabolism)
  • Signal Transduction (drug effects)
  • p38 Mitogen-Activated Protein Kinases (genetics, metabolism)

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