Piperlongumine downregulates the expression of HER family in breast cancer cells

Biochem Biophys Res Commun. 2017 May 13;486(4):1083-1089. doi: 10.1016/j.bbrc.2017.03.166. Epub 2017 Apr 1.

Abstract

HER family receptors are frequently deregulated in breast cancer and the deregulation of these receptors is associated with poor prognosis. Thus, these receptors are considered therapeutic targets. In the present study, we found that piperlongumine (PL) downregulates the expression of HER family receptors HER1, HER2, and HER3 in breast cancer cells. Downregulation of these receptors by PL is mediated through the generation of reactive oxygen species (ROS), as N-acetyl-cysteine blocks it. Interestingly, the HER2-overexpressing cell lines BT474 and SkBr3 are somewhat more sensitive to PL than the low HER2-expressing cell line MCF7. In addition, the overexpression of HER2 increases the sensitivity of MCF7 cells to PL. Collectively, our data indicate the therapeutic potential of PL in the treatment of breast cancer.

Keywords: Breast cancer; HER1; HER2; HER3; Piperlongumine; Reactive oxygen species.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Apoptosis / drug effects
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Dioxolanes / administration & dosage*
  • Dose-Response Relationship, Drug
  • Down-Regulation / drug effects
  • ErbB Receptors / biosynthesis*
  • Gene Expression Regulation, Neoplastic / drug effects*
  • Humans
  • MCF-7 Cells
  • Reactive Oxygen Species / metabolism*

Substances

  • Antineoplastic Agents
  • Dioxolanes
  • Reactive Oxygen Species
  • ErbB Receptors
  • piperlongumine