Apoptotic activities in closely related styryllactone stereoisomers toward human tumor cell lines: Investigation of synergism of styryllactone-induced apoptosis with TRAIL

Bioorg Med Chem. 2010 Jan 15;18(2):849-54. doi: 10.1016/j.bmc.2009.11.045. Epub 2009 Nov 27.

Abstract

A related series of styryllactones with small functional and stereochemical variations were compiled for a comparative study of their apoptotic activities toward two tumorigenic and one non-tumorigenic control cell line. While a substantial range of intrinsic activity was observed, the relative order of activity of the different compounds toward the cell types varied somewhat as did the relative ratios of apoptosis and necrosis observed in conjunction with the loss of cell viability. While some of the styryllactones showed substantial activity, a small but significant apoptosis-induced synergism was demonstrated with (-)-altholactone and TRAIL (tumor necrosis factor-related apoptosis-inducing ligand).

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Cell Survival / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Lactones / chemical synthesis
  • Lactones / chemistry
  • Lactones / pharmacology*
  • Molecular Conformation
  • Stereoisomerism
  • Structure-Activity Relationship
  • TNF-Related Apoptosis-Inducing Ligand / chemistry
  • TNF-Related Apoptosis-Inducing Ligand / metabolism*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Lactones
  • TNF-Related Apoptosis-Inducing Ligand