Identification of Triptophenolide from Tripterygium wilfordii as a Pan-antagonist of Androgen Receptor
Yang He1, Meng Wu1, Yangguang Liu1
1Institute of Medicinal Biotechnology, Chinese Academy of Medical Science , Beijing, China.
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.
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