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.
Diego A Pedroza  1 ,  Fernando De Leon  1 ,  Armando Varela-Ramirez  2 ,  Carolina Lema  2 ,  Renato J Aguilera  3 ,  Shizue Mito  4
Affiliations
  • 1. Department of Chemistry, University of Texas at El Paso, El Paso, TX 79968, USA; Department of Biological Sciences and Border Biomedical Research Center, University of Texas at El Paso, El Paso, TX 79968, USA.
  • 2. Department of Biological Sciences and Border Biomedical Research Center, University of Texas at El Paso, El Paso, TX 79968, USA.
  • 3. Department of Biological Sciences and Border Biomedical Research Center, University of Texas at El Paso, El Paso, TX 79968, USA. Electronic address: [email protected].
  • 4. Department of Chemistry, University of Texas at El Paso, El Paso, TX 79968, USA. Electronic address: [email protected].
PMID: 24368029 DOI: 10.1016/j.bmc.2013.12.007
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.