Novel nitroaromatic compound activates autophagy and apoptosis pathways in HL60 cells

Chem Biol Interact. 2018 Mar 1:283:107-115. doi: 10.1016/j.cbi.2017.12.012. Epub 2017 Dec 6.

Abstract

N-(2-butanoyloxyethyl)-4-(chloromethyl)-3-nitrobenzamide (NBCN) is a nitroaromatic bioreducible compound with cytotoxic effects in cancer cell lines. The aim of this work was to investigate the molecular mechanisms involved in cell death promoted by NBCN in HL60 cells. We observed that NBCN treatment increased intracellular ROS and reduced mitochondria membrane potential (ΔΨm). NBCN treatment also induced morphological changes, phosphatidylserine exposure, cell cycle arrest in G2/M-phase, DNA condensation and fragmentation, but it did not show cytotoxic effects on normal human peripheral blood mononuclear cells (PBMCs). NBCN-induced caspase 3- and 9-dependent DNA fragmentation, which was blocked by pretreatment with the broad-spectrum caspase inhibitor, z-VAD-fmk. Flow cytometry analysis demonstrated that NBCN also increased of the number of autophagic vesicles in HL60 cells, which was not observed when cells were pre-treated with bafilomycin A1. Taken together, these results indicate that NBCN triggered the mitochondrial apoptotic pathway and led to the onset of autophagic cell death, which contributed to its cytotoxic effects.

Keywords: Apoptosis; Autophagy; G2/M arrest; Nitrocompound.

MeSH terms

  • Amino Acid Chloromethyl Ketones / pharmacology
  • Apoptosis / drug effects*
  • Autophagy / drug effects*
  • Benzamidines / chemistry
  • Benzamidines / toxicity*
  • Caspase Inhibitors / pharmacology
  • Caspases / metabolism
  • Cells, Cultured
  • DNA Fragmentation / drug effects
  • G2 Phase Cell Cycle Checkpoints / drug effects
  • HL-60 Cells
  • Humans
  • Leukocytes, Mononuclear / cytology
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / metabolism
  • M Phase Cell Cycle Checkpoints / drug effects
  • Macrolides / pharmacology
  • Membrane Potential, Mitochondrial / drug effects
  • Reactive Oxygen Species / metabolism

Substances

  • Amino Acid Chloromethyl Ketones
  • Benzamidines
  • Caspase Inhibitors
  • Macrolides
  • Reactive Oxygen Species
  • benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone
  • 3-nitrobenzamidine
  • bafilomycin A1
  • Caspases