PMS-1077, a PAF antagonist, induced differentiation of HL-60 cells with its novel activity

Cell Biol Int. 2010 Dec;34(12):1227-30. doi: 10.1042/CBI20100168.

Abstract

The cell differentiation-inducing effect of 2-N,N-diethylaminocarbonyloxymethyl-1-diphenylmethyl-4-(3,4,5-trimethoxybenzoyl) piperazine, hydrochloride (PMS-1077) was determined in human leukaemic HL-60 cells with profiling of cell proliferation, analysis of cell cycling, characterization of expression of various CD molecules and determination of phagocytotic activity of differentiated HL-60 cells. After treatment with PMS-1077, HL-60 cells exhibited a decreased cell viability during which cell cycle was arrested in G₀-/G₁-phase. Flow cytometric analysis showed CD11b and CD14 were up-regulated, whereas CD15 was unaffected. Together with the finding that PMS-1077-treated HL-60 cells exhibited activities of differentiation by examining their ability of phagocytosing latex beads, an antiproliferative effect and a differentiation-inducing role were determined for PMS-1077 in HL-60 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Carbamates / pharmacology*
  • Cell Cycle / drug effects
  • Cell Differentiation / drug effects*
  • Cell Proliferation / drug effects
  • Drug Evaluation, Preclinical
  • HL-60 Cells
  • Humans
  • Lymphocytes / drug effects
  • Lymphocytes / physiology
  • Phagocytosis / drug effects
  • Piperazines / pharmacology*
  • Platelet Activating Factor / antagonists & inhibitors*
  • Platelet Aggregation Inhibitors / pharmacology
  • Up-Regulation / drug effects

Substances

  • 2-N,N-diethylaminocarbonyloxymethyl-1-diphenylmethyl-4-(3,4,5-trimethoxybenzoyl)piperazine
  • Antineoplastic Agents
  • Carbamates
  • Piperazines
  • Platelet Activating Factor
  • Platelet Aggregation Inhibitors