Crispene E, a cis-clerodane diterpene inhibits STAT3 dimerization in breast cancer cells

Org Biomol Chem. 2015 Apr 7;13(13):3882-6. doi: 10.1039/c5ob00052a.

Abstract

Crispene E, a new clerodane-type diterpene, inhibited STAT3 dimerization in a cell-free fluorescent polarisation assay and was found to have significant toxicity against STAT3-dependent MDA-MB 231 breast cancer cell line and selectively inhibited the expression of STAT3 and STAT3 target genes cyclin D1, Fascin and bcl-2. Molecular docking studies suggest the molecule inhibits STAT3 by interacting with its SH2 domain. The compound has been isolated from Tinospora crispa and characterized using standard spectroscopic techniques.

MeSH terms

  • Breast Neoplasms / pathology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Diterpenes, Clerodane / pharmacology*
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Models, Molecular
  • Protein Multimerization / drug effects*
  • Protein Structure, Quaternary
  • STAT3 Transcription Factor / chemistry*
  • STAT3 Transcription Factor / genetics

Substances

  • Diterpenes, Clerodane
  • STAT3 Transcription Factor
  • crispene E