2-Bromopalmitate sensitizes osteosarcoma cells to adriamycin-induced apoptosis via the modulation of CHOP

Eur J Pharmacol. 2019 Feb 5:844:204-215. doi: 10.1016/j.ejphar.2018.12.019. Epub 2018 Dec 12.

Abstract

Osteosarcoma is the most common primary malignant bone tumour, but the survival rate of patients has plateaued since the mid-1980s. Adriamycin is an integral component of the current first-line chemotherapies used for osteosarcoma, but dose-dependent severe side effects often limit its clinical application. Here, we propose a potential combination regimen in which adriamycin plus 2-bromopalmitate, a palmitoylation inhibitor, exhibited powerful therapeutic effects on osteosarcoma. First, 2-bromopalmitate strongly increased the proliferation inhibition of adriamycin in both human osteosarcoma cell lines and primary osteosarcoma cells. Adriamycin-induced apoptosis in osteosarcoma cells was enhanced when synergized with 2-bromopalmitate. Our study indicated that the reactive oxygen species scavenger NAC and GSH could largely reverse the apoptosis induced by adriamycin combined with 2-bromopalmitate, demonstrating that reactive oxygen species played an essential role in this combination therapy. Moreover, CHOP was remarkably elevated in the combination group, and silencing of CHOP almost completely blocked the apoptosis induced by the combination of 2-bromopalmitate and adriamycin. Taken together, our study provides a prospective therapeutic strategy to eliminate osteosarcoma, which is propitious to clinical combination therapy development.

Keywords: 2-Bromopalmitate; Adriamycin; CHOP; Osteosarcoma; Reactive oxygen species.

MeSH terms

  • Adolescent
  • Adult
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Bone Neoplasms / drug therapy
  • Bone Neoplasms / metabolism*
  • Cell Line, Tumor
  • Child
  • Doxorubicin / pharmacology*
  • Drug Synergism
  • Female
  • Humans
  • Osteosarcoma / drug therapy
  • Osteosarcoma / metabolism*
  • Palmitates / pharmacology*
  • Reactive Oxygen Species / metabolism
  • Transcription Factor CHOP / genetics
  • Transcription Factor CHOP / metabolism*
  • Young Adult

Substances

  • Antineoplastic Agents
  • DDIT3 protein, human
  • Palmitates
  • Reactive Oxygen Species
  • Transcription Factor CHOP
  • 2-bromopalmitate
  • Doxorubicin