Diterpenes from Cryptomeria japonica inhibit androgen receptor transcriptional activity in prostate cancer cells

Planta Med. 2007 Oct;73(13):1407-9. doi: 10.1055/s-2007-990233. Epub 2007 Oct 9.

Abstract

We identified eight diterpenes from Cryptomeria japonica (Taxodiaceae), which inhibit the activity of the androgen receptor (AR) in human prostate cancer (PCa) 22Rv1-derived 103E cells. The compounds 6,12-dihydroxyabieta-5,8,11,13-tetraen-7-one ( 2), sugiol ( 3), ferruginol ( 4), and 5-epixanthoperol ( 7) have near 100 % AR inhibition efficacy at concentrations of 10, 5, 25, and 25 microM, respectively. Because these compounds have very similar structures, analysis of their differential activity may aid in the design of inhibitors for PCa treatment.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / administration & dosage
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Antineoplastic Agents, Phytogenic / therapeutic use
  • Cell Line, Tumor / drug effects
  • Cell Line, Tumor / metabolism
  • Cryptomeria*
  • Diterpenes / administration & dosage
  • Diterpenes / pharmacology
  • Diterpenes / therapeutic use
  • Humans
  • Inhibitory Concentration 50
  • Male
  • Phytotherapy*
  • Plant Extracts / administration & dosage
  • Plant Extracts / pharmacology*
  • Plant Extracts / therapeutic use
  • Prostatic Neoplasms / prevention & control
  • Receptors, Androgen / metabolism*

Substances

  • Antineoplastic Agents, Phytogenic
  • Diterpenes
  • Plant Extracts
  • Receptors, Androgen