The cytotoxic effect of 2-acylated-1,4-naphthohydroquinones on leukemia/lymphoma cells

Bioorg Med Chem. 2014 Jan 15;22(2):842-7. doi: 10.1016/j.bmc.2013.12.007. Epub 2013 Dec 11.

Abstract

Here, we tested seven 2-acylated-1,4-hydronaphthoquinones for their cytotoxic effects on a panel of cancer lymphoma/leukemia cells and compared to a non-cancer origin cell line. Several naphthohydroquinones exhibited selective cytotoxic effects on lymphoma/leukemia cells with lowest activity on non-cancer cells. The mode of cell death induced by an acylated naphthohydroquinone, which has a long alkyl chain, was found to be via apoptosis. Furthermore, the naphthohydroquinone provoked mitochondria depolarization and activation of its downstream effector, caspase-3, thus implicating the intrinsic apoptotic pathway as its mechanism to exert cell death.

Keywords: Acylated hydroquinones; Anti-lymphoma; Apoptosis; Cytotoxicity; Photochemistry.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Hydroquinones / chemical synthesis
  • Hydroquinones / chemistry
  • Hydroquinones / pharmacology*
  • Leukemia / drug therapy*
  • Leukemia / pathology
  • Lymphoma / drug therapy*
  • Lymphoma / pathology
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Hydroquinones
  • 1,4-naphthohydroquinone