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Triptophenolide is a diterpenoid that has been found in T. wilfordii and has antiandrogenic activity.1 It is an antagonist of wild-type and mutant androgen receptors (ARs; IC50s = 260, 388, 480, and 437 nM for wild-type, ART877A, ARF876L, and ARW741C/T877A, respectively, in transactivation assays). Triptophenolide (5 µM) inhibits the growth of, and reduces AR levels in, LNCaP prostate cancer cells.
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1. Identification of triptophenolide from Tripterygium wilfordii as a pan-