Lactacystin, a proteasome inhibitor, potentiates the apoptotic effect of parthenolide, an inhibitor of NFkappaB activation, on drug-resistant mouse leukemia L1210 cells

Anticancer Res. 2002 Nov-Dec;22(6C):3805-9.

Abstract

An L1210 cell line (Y8) selected for resistance to deoxyadenosine does not express p53 mRNA or protein but expresses WAF1/p21 even under basal conditions. The Y8 cell line had been previously shown to have an increased apoptotic response to a variety of agents that included DNA damaging agents, kinase inhibitors and drugs directed at NFkappa B activation. In this study we show that lactacystin (LC, an inhibitor of proteasome activity) in combination with parthenolide (PA) caused a synergistic increase in the apoptotic fraction of the Y8 cells. LC (2.5 microM) alone and PA (5.0 microM) caused less than 20% of the Y8 cells to undergo apoptosis. However, the combination of LC (2.5 microM) plus PA (5.0 microM) caused 60% of the Y8 cells to undergo apoptosis. The combination of drugs had no effects on the parental wild-type L1210 cells. Pretreatment of the intact Y8 cells with the caspase-3 inhibitor, Ac-DEVD-CHO, resulted in a marked decrease in the apoptosis caused by the LC plus PA combination. Cell-free extracts prepared from the LC plus PA combination-treated cells had activated caspase activities in the caspase cascade: caspase-3 >> caspase-8 > caspase-6 and caspase-10. These results suggest that there are interacting pathways involving aspects of NFkappa B activation and proteasome activity that could be exploited in therapy directed at p53-deficient tumor cells that would lead to caspase-3 activation and apoptosis bypassing the p53-dependent chemotherapy insensitivity.

MeSH terms

  • Acetylcysteine / analogs & derivatives*
  • Acetylcysteine / pharmacology*
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Apoptosis / drug effects*
  • Caspase 3
  • Caspase Inhibitors
  • Caspases / metabolism
  • Cyclin-Dependent Kinase Inhibitor p21
  • Cyclins / biosynthesis
  • Cysteine Endopeptidases
  • Cysteine Proteinase Inhibitors / pharmacology*
  • Drug Resistance, Neoplasm
  • Drug Synergism
  • Enzyme Activation / drug effects
  • Leukemia L1210 / drug therapy*
  • Leukemia L1210 / metabolism
  • Leukemia L1210 / pathology
  • Mice
  • Multienzyme Complexes / antagonists & inhibitors
  • NF-kappa B / antagonists & inhibitors
  • Proteasome Endopeptidase Complex
  • Sesquiterpenes / pharmacology*
  • Tumor Suppressor Protein p53 / biosynthesis

Substances

  • Caspase Inhibitors
  • Cdkn1a protein, mouse
  • Cyclin-Dependent Kinase Inhibitor p21
  • Cyclins
  • Cysteine Proteinase Inhibitors
  • Multienzyme Complexes
  • NF-kappa B
  • Sesquiterpenes
  • Tumor Suppressor Protein p53
  • lactacystin
  • parthenolide
  • Casp3 protein, mouse
  • Caspase 3
  • Caspases
  • Cysteine Endopeptidases
  • Proteasome Endopeptidase Complex
  • Acetylcysteine