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从灵芝子实体中分离出的灵芝醇B的抗雄激素作用。

The anti-androgen effect of ganoderol B isolated from the fruiting body of Ganoderma lucidum.

作者信息

Liu Jie, Shimizu Kuniyoshi, Konishi Fumiko, Kumamoto Shoichiro, Kondo Ryuichiro

机构信息

Department of Forest and Forest Products Science, Faculty of Agriculture, Kyushu University, Fukuoka 812-8581, Japan.

出版信息

Bioorg Med Chem. 2007 Jul 15;15(14):4966-72. doi: 10.1016/j.bmc.2007.04.036. Epub 2007 Apr 25.

Abstract

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.

摘要

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。

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