Dissociation of the effects of the antitumour ether lipid ET-18-OCH3 on cytosolic calcium and on apoptosis

Br J Pharmacol. 1997 Aug;121(7):1364-8. doi: 10.1038/sj.bjp.0701271.

Abstract

1. We have compared the effects of 1-O-octadecyl-2-O-methyl-sn-glycero-3-phosphocholine (ET-18-OCH3) on the cytosolic free calcium concentration ([Ca2+]i) and on apoptosis in several normal and leukaemia cells, including human polymorphonuclear neutrophils (PMNs), U937 cells, and undifferentiated as well as dimethylsulphoxide-differentiated HL60 cells (uHL60 and dHL60, respectively). 2. ET-18-OCH3 produced apoptosis, as evidenced by DNA degradation into oligonucleosome-size fragments, in U937 and uHL60 cells, but not in dHL60 cells or PMNs. 3. ET-18-OCH3 induced an increase in [Ca2+]i mediated through the platelet-activating factor (PAF) receptor in U937, dHL60 cells and PMNs, as shown by cross-desensitization experiments and by prevention of the [Ca2+]i changes by the PAF antagonist WEB-2170. The EC50 values for the increase in [Ca2+]i induced by PAF and ET-18-OCH3 were 5 x 10(-11) and 2.5 x 10(-7) M, respectively. In uHL60 cells the effect of ET-18-OCH3 on [Ca2+]i was very small and was not affected by WEB-2170. 4. PAF did not produce apoptosis in any of the cell types tested. WEB-2170 did not prevent the apoptosis induced by ET-18-OCH3. 5. The uptake of [3H]-ET-18-OCH3 was much larger in U937 and uHL60 cells than in dHL60 cells and PMNs. 6. Our results indicate that the apoptotic effect of ET-18-OCH3 is not related to the changes in [Ca2+]i, effected by interaction with plasma membrane PAF receptors, but to other actions which are associated with the uptake of this drug into the cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Calcium / metabolism*
  • Cytosol / metabolism
  • HL-60 Cells
  • Humans
  • Phospholipid Ethers / pharmacology*
  • Platelet Activating Factor / pharmacology

Substances

  • Antineoplastic Agents
  • Phospholipid Ethers
  • Platelet Activating Factor
  • edelfosine
  • Calcium