Carcinogenesis Advance Access originally published online on October 17, 2007
Carcinogenesis 2007 28(12):2521-2529; doi:10.1093/carcin/bgm137
| ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Compounds from Wedelia chinensis synergistically suppress androgen activity and growth in prostate cancer cells
1 Agricultural Biotechnology Research Center, Academia Sinica, 128 Academia Road, Sec. 2, Nan-Kang, Taipei 11529, Taiwan
2 Institute of Molecular and Cellular Biology, National Taiwan University, Taipei 10617, Taiwan
* To whom correspondence should be addressed. Tel: +886 2 2651 5747; Fax: +886 2 2785 9360; Email: pwhsiao{at}gate.sinica.edu.tw
Chronic inflammation can augment tumor development in various types of cancers, including prostate cancer (PCa). Reduction of inflammation is therefore an important anticancer therapeutic opportunity. Here, we report four anti-proliferative phytocompounds in Wedelia chinensis, an oriental herbal medicine, identified through their ability to modulate the androgen receptor (AR) activation of transcription from prostate-specific antigen promoter in PCa cells. The 50% inhibition concentration values of indole-3-carboxylaldehyde, wedelolactone, luteolin and apigenin, were 34.9, 0.2, 2.4 and 9.8 µM, respectively. A formula that combined the phytocompounds in the same proportions as in the herbal extract decreased the dosage of each compound required to achieve maximal AR inhibition. In correlation with the AR suppression effect, these active compounds specifically inhibited the growth of AR-dependent PCa cells and as a combination formula they also synergistically suppressed growth in AR-dependent PCa cells. Our study has identified synergistic effects of active compounds in W. chinensis and demonstrated their potential in PCa prevention and therapy. The paradigm of multiple activities and synergism is a useful framework to investigate the therapeutic effects of whole extracts from assorted medicinal plant species.
Abbreviations: Api, apigenin; AR, androgen receptor; CHCl3, chloroform; CI, combination index; DIM, diindolylmethane; EtOAc, ethyl acetate; EtOH, ethanol; H2O-Sub, H2O subfraction; HPLC, high-performance liquid chromatography; IC50, 50% inhibition concentration; ICA, indole-3-carboxylaldehyde; I3C, indole-3-carbinol; Lut, luteolin; PCa, prostate cancer; PSA, prostate-specific antigen; PSA-Luc, prostate-specific antigen-luciferase; Wed, wedelolactone
Received March 23, 2007; revised June 6, 2007; accepted June 6, 2007.
CiteULike 
Connotea 
Del.icio.us What's this?
This article has been cited by other articles:
|
|
 |
|
  C.-H. Tsai, F.-M. Lin, Y.-C. Yang, M.-T. Lee, T.-L. Cha, G.-J. Wu, S.-C. Hsieh, and P.-W. Hsiao Herbal Extract of Wedelia chinensis Attenuates Androgen Receptor Activity and Orthotopic Growth of Prostate Cancer in Nude Mice Clin. Cancer Res., September 1, 2009; 15(17): 5435 - 5444. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 F.-M. Lin, C.-H. Tsai, Y.-C. Yang, W.-C. Tu, L.-R. Chen, Y.-S. Liang, S.-Y. Wang, L.-F. Shyur, S.-C. Chien, T.-L. Cha, et al. A Novel Diterpene Suppresses CWR22Rv1 Tumor Growth In vivo through Antiproliferation and Proapoptosis Cancer Res., August 15, 2008; 68(16): 6634 - 6642. [Abstract] [Full Text] [PDF]
|
|