Chinese Medicines for Prostate Cancer: Do They Activate or Inhibit the Androgen Receptor?
Refereed conference paper presented and published in conference proceedings

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AbstractBackground and Aims:Androgen receptor (AR), located on X chromosome (q11-12), is a 110 kDa nuclear receptor that, upon activation by androgens, mediates transcription of target genes to modulate growth and differentiation of prostate epithelial cells. AR is also the major therapeutic target for the treatment of prostate cancer (PCa). Treatment with anti-androgens, used either singly or combined with other therapies, is highly effective to stabilize the PCa from further progression effectively blocking the endogenous androgen actions via their direct competitive blockade on the AR in prostate cancer cells. Therefore, researchers are increasingly taking an interest in developing potential anti-androgens drugs for use in PCa therapy. Many lines of clinical evidence suggest that Chinese medicine has unique advantage for the treatment of PCa. Bruceae Fructus (BF, 鴉膽子 ) and Hedyotis diffusa Willd (HDW, 白花蛇舌草 ) are among the herbs commonly used in clinical practice for the treatment of PCa. However, mechanism of action underlying the therapeutic efficacy of these herbs for PCa remains largely unknown.
Methods: The LNCaP cells (AR positive PCa cell line) were plated in CS-FBS RPMI 1640 medium in 96-well culture plates and then incubated with above extracts (3.125,, 6.25, 12.5, 25, 50, 100, 200 and 400 μg/mL) in triplicate for 48 h, and MTT assay was used to measure the cell viability.
Results: Our results showed that the IC50 values of Bruceae Fructus (BF, 鴉 膽 子 ), Flemingia philippinensis Merr. et Rolfe (FPMR, 千 斤 拔 ) and Hedyotis diffusa Willd (HDW, 白 花 蛇 舌 草 ) were 15.8±1.02 μg/mL, 156.2±7.3 μg/mL and 166.4±5.6 μg/mL, respectively, in LNCaP cells. In addition, treatment with Persicae Semen (PS, 桃仁 ) or three other herbs for 48 h, the viability of LNCaP cells was markedly reduced in high doses, but the IC50 values were more than 200 μg/mL for the four herbs. On the other hand, Chuanxiong Rhizoma (CR, 川芎 ), together with other twelve herbs at the concentrations up to 200 μg/mL did not show significant cytotoxicity to LNCaP cells when incubated for 48 h.
Conclusions: These results suggested that BF, FP and SHH had severe cytotoxicity to LNCaP cells, while many other selected Chinese herbs in this study had relatively wide margins of safety.
All Author(s) ListZhenbiao Zhang, Yanfang Xian, Paul Siu-Po Ip, Zhixiu Lin
Name of ConferenceInternational Conference on Brain Research in Chinese Medicine: Degeneration and Repair
Start Date of Conference26/07/2018
End Date of Conference28/07/2018
Place of ConferenceHong Kong
Country/Region of ConferenceHong Kong
Proceedings TitleInternational Conference on Brain Research in Chinese Medicine: Degeneration and Repair
LanguagesEnglish-United Kingdom

Last updated on 2019-24-10 at 12:58