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| Bakuchiol inhibits the androgen induced-proliferation of prostate cancer cell line LNCaP through suppression of AR transcription activity |
| Hits 3116 Download times 2175 Received:March 15, 2013 |
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| DOI
10.11656/j.issn.1672-1519.2013.05.13 |
| Key Words
Bakuchiol;prostate cancer;Psoralea corylifolia L.;antagonist of androgen receptor |
| Author Name | Affiliation | | MIAO Lin | Tianjin Key Laboratory of Modern Chinese Medicine, Tianjin University of TCM, Tianjin 300193, China
Tianjin Key Laboratory of Chinese Medical Pharmacology, Tianjin University of TCM, Tianjin 300193, China | | MA Shang-wei | Tianjin Key Laboratory of Chinese Medical Pharmacology, Tianjin University of TCM, Tianjin 300193, China | | FAN Guan-wei | Tianjin Key Laboratory of Chinese Medical Pharmacology, Tianjin University of TCM, Tianjin 300193, China | | WANG Hong | Tianjin Key Laboratory of Modern Chinese Medicine, Tianjin University of TCM, Tianjin 300193, China | | WANG Yue-fei | Tianjin Key Laboratory of Modern Chinese Medicine, Tianjin University of TCM, Tianjin 300193, China | | CHAI Li-juan | Tianjin Key Laboratory of Modern Chinese Medicine, Tianjin University of TCM, Tianjin 300193, China |
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| Abstract
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| [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. [Results] The IC50 of 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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