Curcumin analogues with high activity for inhibiting human prostate cancer cell growth and androgen receptor activation

Mol Med Rep. 2014 Sep;10(3):1315-22. doi: 10.3892/mmr.2014.2380. Epub 2014 Jul 14.


The androgen receptor (AR) has a critical role in prostate cancer development and progression. Several curcumin analogues (A10, B10, C10, E10 and F10) with different linker groups were investigated for their effects in human prostate cancer CWR‑22Rv1 and LNCaP cell lines. The ability of these compounds to inhibit testosterone (TT)‑ or dihydrotestosterone (DHT)‑induced AR activity was determined by an AR‑linked luciferase assay and by TT‑ or DHT‑induced expression of prostate specific antigen. Compounds F10 and E10 had stronger inhibitory effects on the growth of cultured CWR‑22Rv1 and LNCaP cell lines, and they also had enhanced stimulatory effects on apoptosis compared with curcumin and other curcumin analogues (A10, B10, C10) in CWR‑22Rv1 cells. E10 and F10 were more potent inhibitors of AR activity than curcumin, A10 and B10. The higher activities of E10 and F10 may be correlated with a heteroatom linker. The results indicate that one of the potential mechanisms for the anticancer effect of the curcumin analogues was inhibition of AR pathways in human prostate cancer cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Curcumin / analogs & derivatives
  • Curcumin / pharmacology*
  • Dihydrotestosterone / antagonists & inhibitors
  • Dihydrotestosterone / metabolism
  • Humans
  • Male
  • Prostate-Specific Antigen / genetics
  • Prostate-Specific Antigen / metabolism
  • Prostatic Neoplasms / metabolism
  • Receptors, Androgen / genetics
  • Receptors, Androgen / metabolism*
  • Signal Transduction
  • Testosterone / antagonists & inhibitors
  • Testosterone / metabolism


  • AR protein, human
  • Antineoplastic Agents
  • Receptors, Androgen
  • Dihydrotestosterone
  • Testosterone
  • Prostate-Specific Antigen
  • Curcumin