Induction of necrosis in human myeloma cells by kigamicin

Anticancer Res. 2008 Jan-Feb;28(1A):37-43.

Abstract

Background: Kigamicin (KGM) is a novel compound derived from Actinomycetes that was originally reported to induce necrosis in pancreatic cancer cells only under nutrient-starved conditions via inhibition of PI3-kinase. The effects of KGM on myeloma cells were investigated.

Materials and methods: Cytotoxic activity was quantified using WST8 assay. Necrosis was determined by Annexin V/PI staining. Regulatory protein levels were assessed by Western blot. LY294002 was utilized as a PI3-kinase inhibitor.

Results: KGM induced necrosis in myeloma cells in nutrient rich conditions with a CC50 of approximately 100 nM. KGM did not induce necrosis in normal lymphocytes. Cyclin D1, p21, p-AKT and p-ERK were inhibited by KGM while LY294002 did not inhibit cell death by KGM. A melphalan-resistant myeloma cell line was more susceptible to KGM than the melphalan-sensitive parental cell line.

Conclusion: KGM-induced necrosis in myeloma cells even at very low concentration. The present data warrant further investigation into the use of KGM as a potential therapeutic agent for multiple myeloma.

MeSH terms

  • Antibiotics, Antineoplastic / pharmacology*
  • Cell Cycle Proteins / metabolism
  • Doxorubicin / analogs & derivatives*
  • Doxorubicin / pharmacology
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • Humans
  • Lymphocytes / drug effects
  • Multiple Myeloma / blood
  • Multiple Myeloma / drug therapy*
  • Multiple Myeloma / metabolism
  • Multiple Myeloma / pathology
  • Necrosis
  • Oxazoles / pharmacology*
  • Phosphorylation

Substances

  • Antibiotics, Antineoplastic
  • Cell Cycle Proteins
  • Oxazoles
  • kigamicin A
  • Doxorubicin
  • Extracellular Signal-Regulated MAP Kinases