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具有雌激素和雄激素活性的化合物可抑制雌激素/雄激素诱导的前列腺增生过程。

Compounds from with Estrogenic and Androgenic Activities Suppress the Oestrogen/Androgen-Induced BPH Process.

作者信息

Wang Xueni, Tao Rui, Yang Jing, Miao Lin, Wang Yu, Munyangaju Jose Edouard, Wichai Nuttapong, Wang Hong, Zhu Yan, Liu Erwei, Chang Yanxu, Gao Xiumei

机构信息

Tianjin State Key Laboratory of Modern Chinese Medicine, 312 Anshanxi Road, Nankai District, Tianjin 300193, China.

Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, 312 Anshanxi Road, Nankai District, Tianjin 300193, China.

出版信息

Evid Based Complement Alternat Med. 2017;2017:6438013. doi: 10.1155/2017/6438013. Epub 2017 May 15.

Abstract

OBJECTIVE

To investigate the phytoestrogenic and phytoandrogenic activities of compounds isolated from CS and uncover the role of CS in prevention of oestrogen/androgen-induced BPH.

METHODS

Cells were treated with CS compounds, and immunofluorescence assay was performed to detect the nuclear translocation of ER or AR in MCF-7 or LNCaP cells; luciferase reporter assay was performed to detect ERs or AR transcriptional activity in HeLa or AD293 cells; MTT assay was performed to detect the cell proliferation of MCF-7 or LNCaP cells. Oestrogen/androgen-induced BPH model was established in rat and the anti-BPH, anti-estrogenic, and anti-androgenic activities of CS in vivo were further investigated.

RESULTS

The nuclear translocation of ER was stimulated by nine CS compounds, three of which also stimulated AR translocation. The transcriptional activities of ER and ER were induced by five compounds, within which only ECG induced AR transcriptional activity as well. Besides, ECG stimulated the proliferation of both MCF-7 cells and LNCaP cells. CS extract suppressed oestrogen/androgen-induced BPH progress in vivo by downregulation of E2 and T level in serum and alteration of the expressions of ER, ER, and AR in the prostate.

CONCLUSION

Our data demonstrates that compounds from CS exhibit phytoestrogenic and phytoandrogenic activities, which may contribute to inhibiting the oestrogen/androgen-induced BPH development.

摘要

目的

研究从CS中分离出的化合物的植物雌激素和植物雄激素活性,并揭示CS在预防雌激素/雄激素诱导的前列腺增生中的作用。

方法

用CS化合物处理细胞,进行免疫荧光分析以检测MCF-7或LNCaP细胞中雌激素受体(ER)或雄激素受体(AR)的核转位;进行荧光素酶报告基因分析以检测HeLa或AD293细胞中ER或AR的转录活性;进行MTT分析以检测MCF-7或LNCaP细胞的增殖。在大鼠中建立雌激素/雄激素诱导的前列腺增生模型,并进一步研究CS在体内的抗前列腺增生、抗雌激素和抗雄激素活性。

结果

9种CS化合物刺激了ER的核转位,其中3种还刺激了AR转位。5种化合物诱导了ER和雌激素相关受体(ER)的转录活性,其中只有表儿茶素(ECG)也诱导了AR转录活性。此外,ECG刺激了MCF-7细胞和LNCaP细胞的增殖。CS提取物通过下调血清中雌二醇(E2)和睾酮(T)水平以及改变前列腺中ER、ER和AR的表达,在体内抑制雌激素/雄激素诱导的前列腺增生进展。

结论

我们的数据表明,CS中的化合物具有植物雌激素和植物雄激素活性,这可能有助于抑制雌激素/雄激素诱导的前列腺增生发展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2966/5447316/f373c982162f/ECAM2017-6438013.001.jpg

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