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Bakuchiol inhibits the androgen induced-proliferation of prostate cancer cell line LNCaP through suppression of AR transcription activity

MIAO Lin1,2,MA Shang-wei2,FAN Guan-wei2,WANG Hong1,WANG Yue-fei1,CHAI Li-juan1(1.Tianjin Key Laboratory of Modern Chinese Medicine,Tianjin University of TCM,Tianjin 300193,China;2.Tianjin Key Laboratory of Chinese Medical Pharmacology,Tianjin University of TCM,Tianjin 300193,China)  
[Objective] To explore the effect of bakuchiol on the affinity and transcription activity of androgen receptor(AR),and by which bakuchiol behaviors in the androgen-dependent PCa cell line LNCaP.[Methods] AR competitor binding assay was used to detect the affinity of bakuchiol to AR.Luciferase reporter assay was used to detect the effect of bakuchiol on testosterone-induced AR transcription activity.LNCaP cells were treated with bakuchiol and/or testosterone and the expression of androgen targeted gene prostate specific antigen(PSA) and the cell proliferation induced by testosterone were then detemined by real-time PCR and MTT assay.[Resnlts] The IC50of bakuchiol to AR is 8.87×104,which is similar with flutamide(10.00×104).Bakuchiol effectively blocked testosterone-induced AR transcription activity.The PSA expression and cell proliferation induced by testosterone in LNCaP were significantly inhibited by bakuchiol.[Conclusion] Bakuchiol suppressed testosterone-induced cell proliferation and gene expression in LNCaP by targeting AR,which indicates a potential usefulness of bakuchiol as an AR antagonist for drug development and treatment of androgen-dependent PCa.
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