Cryptotanshinone inhibits breast cancer cell growth by suppressing estrogen receptor signaling
Cryptotanshinone inhibits breast cancer cell growth by suppressing estrogen receptor signaling
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隐丹参酮通过抑制雌激素受体信号传导来抑制乳腺癌细胞生长。
DOI：
10.4161/15384047.2014.962960
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发表时间：
2015-01-01
影响因子：
3.6
通讯作者：
Zhou, Jianguang
中科院分区：
文献类型：
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作者：
Li, Shanhu;Wang, Hongtao;Zhou, Jianguang
雌激素受体（ER）是乳腺癌治疗的主要靶点，因为雌激素信号失调在乳腺癌的发生和发展中起着至关重要的作用。在这项研究中，我们报告了一个新的ER结合化合物，隐丹参酮（CPT），通过筛选CADD数据库。我们还表明，CPT有效地抑制雌激素诱导的ER反式激活和ER靶基因的基因表达。此外，我们发现CPT主要以ER依赖的方式抑制乳腺癌细胞的生长。最后，我们通过体内异种移植实验证实了CPT的潜在治疗效果。综上所述，我们的研究结果描述了CPT抗癌活性的新机制，并为其作为治疗ER阳性乳腺癌患者的潜在治疗药物提供了支持证据。
Estrogen receptor (ER) is a major therapeutic target for the treatment of breast cancer, because of the crucial role of estrogen signaling deregulation in the development and progression of breast cancer. In this study, we report the identification of a novel ER binding compound, cryptotanshinone (CPT), by screening the CADD database. We also show that CPT effectively inhibits estrogen-induced ER transactivation and gene expression of ER target genes. Furthermore, we showed that CPT suppressed breast cancer cell growth mainly in an ER dependent manner. Finally, we confirmed the potential therapeutic efficiency of CPT using xenograft experiments in vivo. Taken together, our results describe a novel mechanism for the anticancer activity of CPT and provide supporting evidence for its use as a potential therapeutic agent to treat patients with ER positive breast cancer.