Anti-neuroblastoma activity of Helminthosporium carbonum (HC)-toxin is superior to that of other differentiating compounds in vitro

Cancer Lett. 2008 Jun 8;264(1):21-8. doi: 10.1016/j.canlet.2008.01.002. Epub 2008 Feb 8.

Abstract

Treatment of high-risk neuroblastoma (NB) is difficult. Novel therapeutics improving survival rates are urgently required. We have previously shown that the histone deacetylase inhibitor (HDACI) Helminthosporium carbonum (HC)-toxin induces differentiation of neuroblastoma (NB) cells. Here, we show that HC-toxin inhibits the growth of both established NB cell lines and primary cultures with and without amplified MYCN stronger than retinoids (RAs) and other HDACIs (MS-275, n-butyric acid, suberoylanilide hydroxamic acid, trichostatin A, valproic acid). Nanomolar dosages suppress E2F-1, N-myc, Skp2, Mad2 and survivin proteins, found at high levels in high-risk NBs, more efficiently than both RAs and other HDACIs. The level of hypophosphorylated active retinoblastoma (RB) tumor suppressor protein is increased most effectively. HC-toxin's epoxy group is essential for inhibiting HDACs and promoting anti-NB activity. Without this functional group, those cellular effects are not observed. In conclusion, the anti-NB activity of HC-toxin is superior to that of RAs and that of all other HDACIs tested.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Cell Cycle / drug effects
  • Cell Differentiation / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Helminthosporium* / chemistry
  • Histone Deacetylase Inhibitors
  • Humans
  • Inhibitory Concentration 50
  • Mycotoxins / pharmacology*
  • Neuroblastoma / drug therapy*
  • Neuroblastoma / metabolism
  • Peptides, Cyclic / pharmacology*
  • Phosphorylation / drug effects
  • Retinoblastoma Protein / drug effects
  • Retinoblastoma Protein / metabolism
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors
  • Mycotoxins
  • Peptides, Cyclic
  • Retinoblastoma Protein
  • HC toxin