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通过调节22Rv1前列腺癌细胞中的PSA和KLK2发挥雄激素活性。

Exerts Androgenic Activity via Regulation of PSA and KLK2 in 22Rv1 Prostate Cancer Cells.

作者信息

Jeong Soo-Jin, Choi Ji-Yoon, Dong Mi-Sook, Seo Chang-Seob, Shin Hyeun-Kyoo

机构信息

KM Convergence Research Division, Korea Institute of Oriental Medicine, Deajeon, Republic of Korea; Korean Medicine Life Science, University of Science and Technology, Daejeon, Republic of Korea.

School of Life Sciences and Biotechnology, Korea University, Seoul, Republic of Korea.

出版信息

Pharmacogn Mag. 2017 Jan-Mar;13(49):153-158. doi: 10.4103/0973-1296.197657.

Abstract

BACKGROUND

The androgen comprises a group of hormones that play roles in male reproductive activity as well as personal characteristics.

OBJECTIVE

We investigated the androgenic activity of various herbal medicines in human prostate cancer 22Rv1 cells.

MATERIALS AND METHODS

Herbal extracts of (TK), (AS), (SO), and (XS) were selected to have androgenic effects based on a preliminary screening system.

RESULTS

TK, AS, SO, and XS enhanced the proliferation of 22Rv1 cells without having cytotoxic effects. All tested herbal extracts increased androgen receptor (AR)-induced transcriptional activity in the absence or presence of dihydrotestosterone (DHT). In an AR-binding assay, TK, but not AS, SO, or XS, produced a significant inhibition of AR binding activity, indicating it has androgenic activity. Additionally, TK treatment positively regulated mRNA expression of the AR-related molecular targets prostate-specific antigen (PSA) and kallikrein 2 (KLK2) compared with untreated control.

CONCLUSION

Taken together, TK-enhanced AR-mediated transcriptional activity might be an attractive candidate drug for treating androgen-related diseases.

SUMMARY

Trichosantheskirilowii (TK), Asarumsieboldii (AS), Sanguisorbaofficinalis (SO), and Xanthium strumarium (XS) enhanced the proliferation of 22Rv1 cells without having cytotoxic effects.TK, AS, SO, and XS increased androgen receptor (AR)-induced transcriptional activity.TK, but not AS, SO, or XS, produced a significant inhibition against AR-binding activity.TK treatment positively regulated mRNA expression of the AR-related molecular targets prostate-specific antigen and kallikrein 2. BPH: benign prostatic hyperplasia; AR: androgen receptor; DHT: dihydrotestosterone; PSA: prostate-specific antigen; TK: Trichosanthes kirilowii; AS: Asarum sieboldii; SO: Sanguisorba officinalis; XS: Xanthium strumarium; ATCC: American Type Culture Collection; FBS: fetal bovine serum; PBS: phosphate-buffered saline; SD: standard deviation; ARE: androgenresponsive element; KLK: kallikrein.

摘要

背景

雄激素是一类在男性生殖活动及个人特征方面发挥作用的激素。

目的

我们研究了多种草药在人前列腺癌22Rv1细胞中的雄激素活性。

材料与方法

基于初步筛选系统,选择栝楼(TK)、细辛(AS)、地榆(SO)和苍耳(XS)的草药提取物具有雄激素作用。

结果

TK、AS、SO和XS可增强22Rv1细胞的增殖且无细胞毒性作用。所有测试的草药提取物在存在或不存在二氢睾酮(DHT)的情况下均增加雄激素受体(AR)诱导的转录活性。在AR结合试验中,TK而非AS、SO或XS对AR结合活性产生显著抑制,表明其具有雄激素活性。此外,与未处理的对照相比,TK处理正向调节AR相关分子靶点前列腺特异性抗原(PSA)和激肽释放酶2(KLK2)的mRNA表达。

结论

综上所述,TK增强的AR介导的转录活性可能是治疗雄激素相关疾病的有吸引力的候选药物。

总结

栝楼(TK)、细辛(AS)、地榆(SO)和苍耳(XS)可增强22Rv1细胞的增殖且无细胞毒性作用。TK、AS、SO和XS增加雄激素受体(AR)诱导的转录活性。TK而非AS、SO或XS对AR结合活性产生显著抑制。TK处理正向调节AR相关分子靶点前列腺特异性抗原和激肽释放酶2的mRNA表达。BPH:良性前列腺增生;AR:雄激素受体;DHT:二氢睾酮;PSA:前列腺特异性抗原;TK:栝楼;AS:细辛;SO:地榆;XS:苍耳;ATCC:美国典型培养物保藏中心;FBS:胎牛血清;PBS:磷酸盐缓冲盐水;SD:标准差;ARE:雄激素反应元件;KLK:激肽释放酶

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c18/5307901/04156c5890d9/PM-13-153-g001.jpg

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