Identification of Triptophenolide from Tripterygium wilfordii as a Pan-antagonist of Androgen Receptor

  • ACS Med Chem Lett. 2016 Sep 28;7(12):1024-1027. doi: 10.1021/acsmedchemlett.6b00180.
Yang He  1 ,  Meng Wu  1 ,  Yangguang Liu  1 ,  Quanjie Li  1 ,  Xiaoyu Li  1 ,  Laixing Hu  1 ,  Shan Cen  1 ,  Jinming Zhou  1
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Science , Beijing, China.
PMID: 27994731 DOI: 10.1021/acsmedchemlett.6b00180
Abstract

A compound, triptophenolide, derived from Tripterygium wilfordii was identified as an antiandrogen. Triptophenolide inhibits the activity of both wild-type and F876L mutant androgen receptors. Triptophenolide exhibits its antiandrogenic activity through competitive binding with androgen in the hormone-binding pocket, decreasing the expression of Androgen Receptor, and reducing the nuclear translocation of Androgen Receptor.

Keywords
Androgen receptor; gene report system; traditional Chinese medicine; triptophenolide.
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