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. 2016 Sep 28;7(12):1024–1027. doi: 10.1021/acsmedchemlett.6b00180

Figure 1.

Figure 1

Triptophenolide is identified as an antiandrogen: (A) Effect of triptophenolide on wild-type AR activity in PC-3 cells. (B) Effect of triptophenolide on F876L AR activity in PC-3 cells. The F876L mutated AR was activated by ENZ at 500 nM. (C) Effect of triptophenolide on T877A AR activity in PC-3 cells. The T877A mutated AR was activated by hydroxyflutamide at 5 μM. (D) Effect of triptophenolide on T877A+W741C AR activity in PC-3 cells. The T877A + W741C mutated AR was activated by both hydroxyflutamide and bicalutamide at 5 μM. (E) Triptophenolide significantly downregulated PSA mRNA level at 500 nM and 5 μM. (F) Growth inhibitory effects of triptophenolide in the PC-3 and LNCaP cells. Plasmids expressing ARs are transiently transfected in PC-3 cells in dual luciferase assay. Experiments were in triplicate. *P < 0.05, **P < 0.01, ***P < 0.001 vs DMSO group, △P < 0.05, △△P < 0.01, △△△ P < 0.001 vs DHT group. BIC, bicalutamide; ENZ, enzalutamide; DHT, dihydrotestosterone. All results are shown as mean ± SD.