Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan-antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild-type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate-specific antigen mRNA levels, and suppresses the growth of AR-positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer[1][2][3].
