Liu Jie, Shimizu Kuniyoshi, Konishi Fumiko, Kumamoto Shoichiro, Kondo Ryuichiro
Department of Forest and Forest Products Science, Faculty of Agriculture, Kyushu University, Fukuoka 812-8581, Japan.
Bioorg Med Chem. 2007 Jul 15;15(14):4966-72. doi: 10.1016/j.bmc.2007.04.036. Epub 2007 Apr 25.
The anti-androgenic activity of the ethanol extract of the fruiting body of Ganoderma lucidum has been previously reported. Ganoderol B with 5alpha-reductase inhibitory activity and the ability to bind to androgen receptor (AR) can inhibit androgen-induced LNCaP cell growth and suppress regrowth of the ventral prostate induced by testosterone in rats. The down-regulation of AR signaling by ganoderol B provides an important mechanism for its anti-androgenic activity. In view of the fact that PSA (prostatic specific antigen, a well-accepted prognostic indicator of prostate cancer) is down-regulated, an important implication of this study is that ganoderol B intervention strategy aimed at toning down the amplitude of androgen signaling could be helpful in controlling morbidity of prostate cancer. In conclusion, our result suggests that ganoderol B might be useful in prostate cancer and benign prostatic hyperplasia (BPH) therapy through suppressing the function of androgen and its receptor.
此前已有报道灵芝子实体乙醇提取物的抗雄激素活性。具有5α-还原酶抑制活性且能与雄激素受体（AR）结合的灵芝醇B可抑制雄激素诱导的LNCaP细胞生长，并抑制大鼠睾丸酮诱导的前列腺腹侧叶再生长。灵芝醇B对AR信号的下调为其抗雄激素活性提供了重要机制。鉴于前列腺特异性抗原（PSA，一种被广泛认可的前列腺癌预后指标）下调，本研究的一个重要意义在于，旨在降低雄激素信号幅度的灵芝醇B干预策略可能有助于控制前列腺癌的发病率。总之，我们的结果表明，灵芝醇B可能通过抑制雄激素及其受体的功能，对前列腺癌和良性前列腺增生（BPH）治疗有用。
