Androprostamines A and B, the new anti-prostate cancer agents produced by Streptomyces sp. MK932-CF8.

Androprostamines A and B, the new anti-prostate cancer agents produced by Streptomyces sp. MK932-CF8.
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雄前列胺 A 和 B,是由链霉菌属 (Streptomyces sp.) 产生的新型抗前列腺癌药物。

DOI:
10.1038/ja.2014.135
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发表时间:
2015
期刊:
J. Antibiot.
影响因子:
--
通讯作者:
Nomoto A.
Nomoto A.
中科院分区:
--
文献类型:
--
作者:
Yamazaki Y;Someno T;Igarashi M;Kinoshita N;Hatano M;Kawada M;Momose I;Nomoto A.

文献摘要

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雄激素受体(AR)在前列腺癌的所有临床状态中都是一个有效的靶点。从Streptomyces sp. MK932-CF8中分离到新的雄激素受体抑制剂雄prostamines A和B。通过光谱分析、降解研究和合成确定了它们的结构。雄prostamines对雄激素依赖性的人前列腺癌细胞的生长有明显的抑制作用,但没有细胞毒性,并抑制雄激素诱导的ar调节基因的表达。
Androgen receptor (AR) is a validated target in all clinical states of prostate cancer. Androprostamines A and B, the new inhibitors of androgen receptor, were isolated from Streptomyces sp. MK932-CF8. Their structures were determined by the spectroscopic analysis, degradation studies and synthesis. Androprostamines showed potent inhibitory effect against androgen-dependent growth of human prostate cancer cells without cytotoxicity and repressed the androgen-induced expression of AR-regulated genes.