Liposomal ET-18-OCH(3) induces cytochrome c-mediated apoptosis independently of CD95 (APO-1/Fas) signaling

Blood. 1999 Nov 15;94(10):3583-92.

Abstract

ELL-12, a liposome formulation of the ether-lipid 1-O-octadecyl-2-O-methyl-sn-glycero-3-phosphocholine (ET-18-OCH(3)), is a nonmyelosuppressive antiproliferative agent that is more effective and less toxic than the ether lipid itself in tumor model systems. We found that ELL-12 induced apoptosis in Jurkat, H9, and U-937 cells that was preceded by activation of executioner caspases. In addition, ELL-12 triggered release of cytochrome c from mitochondria to the cytoplasm before caspase-9 activation. Apoptosis, activation of caspases, and cytochrome c release were blocked by Bcl-x(L) overexpression in Jurkat T cells, suggesting a critical role for mitochondria in ELL-12-triggered cell death. Furthermore, ELL-12 had no effect on expression of CD95 ligand, and inhibition of the Fas signaling pathway with antagonistic anti-CD95 antibody did not affect apoptosis induced by ELL-12. Hence, ELL-12 could be a promising adjunct for the treatment of tumors in addition to myelosuppressive chemotherapeutic drugs and/or those that use the CD95-ligand/receptor system to trigger apoptosis.

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis*
  • Biological Transport
  • Caspases / metabolism
  • Cytochrome c Group / metabolism*
  • Cytochrome c Group / physiology
  • Cytosol / metabolism
  • Dose-Response Relationship, Drug
  • Drug Carriers
  • Drug Delivery Systems
  • Enzyme Activation
  • Humans
  • Jurkat Cells
  • Lamins
  • Liposomes
  • Mitochondria / metabolism
  • Nuclear Proteins / metabolism
  • Peptide Hydrolases / metabolism
  • Phospholipid Ethers / pharmacology*
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Signal Transduction
  • Time Factors
  • U937 Cells
  • bcl-X Protein
  • fas Receptor / metabolism*

Substances

  • Antineoplastic Agents
  • BCL2L1 protein, human
  • Cytochrome c Group
  • Drug Carriers
  • Lamins
  • Liposomes
  • Nuclear Proteins
  • Phospholipid Ethers
  • Proto-Oncogene Proteins c-bcl-2
  • bcl-X Protein
  • fas Receptor
  • edelfosine
  • Peptide Hydrolases
  • Caspases
  • DEVDase