The estrogenic properties of Danggui Buxue Tang, a Chinese herbal decoction, are triggered predominantly by calycosin in MCF-7 cells
The estrogenic properties of Danggui Buxue Tang, a Chinese herbal decoction, are triggered predominantly by calycosin in MCF-7 cells
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当归补血汤在MCF-7细胞中的雌激素样作用主要由毛蕊异黄酮触发
DOI：
10.1016/j.jep.2016.05.035
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发表时间：
2016-08-02
影响因子：
5.4
通讯作者：
Tsim, Karl W. K.
中科院分区：
文献类型：
--
作者：
Gong, Amy G. W.;Lau, Kei M.;Tsim, Karl W. K.
背景：当归补血汤（DBT）是以黄芪（Astragalus memebranaceus（菲施.）邦吉湾mongholicus（Bunge）Hsiao）和当归（ASR; Angelica sinensis Oliv.）重量比为5：1，用于改善妇女的更年期综合症。有证据表明DBT具有很强的雌激素样作用，但其作用机制尚不清楚。毛蕊异黄酮是AR中的主要黄酮类化合物，与β-雌二醇具有相似的结构，因此被推测为DBT中负责这些雌激素活性的关键化合物。目的：我们旨在通过建立去除毛蕊异黄酮的DBT来确定毛蕊异黄酮在DBT中的雌激素活性方面的作用方法：在培养的MCF-7细胞中，通过测定以下参数来比较由DBT Delta cal、DBT+cal和亲本DBT触发的信号传导：（i）雌激素反应元件的激活;（ii）雌激素受体α（ER α）的磷酸化;和（iii）Erk 1/2的磷酸化。DBT诱导的反应呈剂量和/或时间依赖性。结果：DBT Delta Cal中DBT触发的雌激素信号明显减少，相比之下，DBT中添加毛蕊异黄酮（即DBT+Cal）使反应增强2-5倍;然而，单独的毛蕊异黄酮并未表现出此类特性。在平行，DBT诱导的反应可以显着阻断抑制剂雌激素受体和丝裂原活化蛋白kinases.Conclusion：因此，我们假设毛蕊异黄酮是一个不可缺少的化学DBT，并在编排多个组件的DBT发挥连接器，以实现最大的雌激素功能。这些发现对药物开发和从新的角度研究中药现代化具有重要意义。(C)2016爱思唯尔爱尔兰有限公司版权所有。
Background: Danggui Buxue Tang (DBT), a Chinese herbal decoction containing Astragali Radix (AR; roots of Astragalus memebranaceus (Fisch.) Bunge var. mongholicus (Bunge) Hsiao) and Angelicae Sinensis Radix (ASR; roots of Angelica sinensis Oliv.) at a weight ratio of 5:1, is used to improve menopausal syndromes in women. Several lines of evidence indicate that DBT has strong estrogenic property; however, the action mechanism of this herbal decoction is not known. Calycosin, a major flavonoid in AR, shares similar structure with beta-estradiol, and thus which is hypothesized to be the key compound of DBT in responsible for such estrogenic properties.Aims: We aimed to determine the role of calycosin in DBT in terms of its estrogenic functions by the creation of calycosin-depleted DBT (DBT Delta cal) and calycosin-added DBT (DBT+cal) herbal extracts.Methods: The signalings triggered by DBT Delta cal, DBT+cal, and parental DBT were compared in cultured MCF-7 cells by determining: (i) the activation of estrogen responsive element; (ii) the phosphorylation of estrogen receptor a (ER alpha); and (iii) the phosphorylation of Erk1/2. The DBT-induced responses were in dose-and/or time-dependent manners.Results: The estrogenic signals triggered by DBT were markedly reduced in DBT Delta cal, and in contrast the addition of calycosin in DBT, i.e. DBT+cal, enhanced the responses by 2-5 folds; however, calycosin alone did not show such properties. In parallel, the DBT-induced responses could be significantly blocked by inhibitors for estrogen receptor and mitogen activated protein kinases.Conclusion: Thus, we hypothesize that calycosin is an indispensable chemical in DBT, and which plays a linker in orchestrating multi-components of DBT as to achieve the maximal estrogenic functions. These discoveries should be invaluable in drug development and in investigating the modernization of traditional Chinese medicine from a new perspective. (C) 2016 Elsevier Ireland Ltd. All rights reserved.