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.

中文翻译：

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雷公藤雷公藤多酚类化合物作为雄激素受体的全拮抗药的鉴定

源自雷公藤的化合物雷公藤多酚被鉴定为抗雄激素。雷公藤甲酚同时抑制野生型和F876L突变雄激素受体的活性。雷公藤甲内酯通过与荷尔蒙结合袋中的雄激素竞争性结合，降低雄激素受体的表达并减少雄激素受体的核易位，表现出其抗雄激素活性。