Cytotoxic activity of rearranged drimane meroterpenoids against colon cancer cells via down-regulation of β-catenin expression

J Nat Prod. 2015 Mar 27;78(3):453-61. doi: 10.1021/np500843m. Epub 2015 Jan 15.

Abstract

Colorectal cancer has emerged as a major cause of death in Western countries. Down-regulation of β-catenin expression has been considered a promising approach for cytotoxic drug formulation. Eight 4,9-friedodrimane-type sesquiterpenoids (1-8) were acquired using the oxidative potential of Verongula rigida on bioactive metabolites from two Smenospongia sponges. Compounds 3 and 4 contain a 2,2-dimethylbenzo[d]oxazol-6(2H)-one moiety as their substituted heterocyclic residues, which is unprecedented in such types of meroterpenoids. Gauge-invariant atomic orbital NMR chemical shift calculations were employed to investigate stereochemical details with support of the application of advanced statistics such as CP3 and DP4. Compounds 2 and 8 and the mixture of 3 and 4 suppressed β-catenin response transcription (CRT) via degrading β-catenin and exhibited cytotoxic activity on colon cancer cells, implying that their anti-CRT potential is, at least in part, one of their underlying antineoplastic mechanisms.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification*
  • Antineoplastic Agents / pharmacology
  • Colonic Neoplasms / drug therapy*
  • Down-Regulation / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Polycyclic Sesquiterpenes
  • Sesquiterpenes
  • Terpenes / chemistry
  • Terpenes / isolation & purification*
  • Terpenes / pharmacology*
  • beta Catenin / drug effects
  • beta Catenin / genetics*

Substances

  • Antineoplastic Agents
  • Polycyclic Sesquiterpenes
  • Sesquiterpenes
  • Terpenes
  • beta Catenin
  • drimane