Salvianolic Acid A, as a Novel ETA Receptor Antagonist, Shows Inhibitory Effects on Tumor in Vitro
文献类型：期刊论文
| 作者 | Zhang, Qiao2; Wang, Shifeng2; Yu, Yangyang2; Sun, Shengnan3; Zhang, Yuxin2; Zhang, Yanling2; Yang, Wei1; Li, Shiyou4; Qiao, Yanjiang2 |
| 刊名 | International journal of molecular sciences
 |
| 出版日期 | 2016-08-02 |
| 卷号 | 17期号:8 |
| ISSN号 | 1422-0067 |
| DOI | 10.3390/ijms17081244 |
| 文献子类 | Article |
| 英文摘要 | Endothelin-1 (ET-1) autocrine and paracrine signaling modulate cell proliferation of tumor cells by activating its receptors, endothelin A receptor (ETAR) and endothelin B receptor (ETBR). Dysregulation of ETAR activation promotes tumor development and progression. The potential of ETAR antagonists and the dual-ETAR and ETBR antagonists as therapeutic approaches are under preclinical and clinical studies. Salvianolic acid A (Sal A) is a hydrophilic polyphenolic derivative isolated from Salvia miltiorrhiza Bunge (Danshen), which has been reported as an anti-cancer and cardio-protective herbal medicine. In this study, we demonstrate that Sal A inhibits ETAR activation induced by ET-1 in both recombinant and endogenous ETAR expression cell lines. The IC50 values were determined as 5.7 µM in the HEK293/ETAR cell line and 3.14 µM in HeLa cells, respectively. Furthermore, our results showed that Sal A suppressed cell proliferation and extended the doubling times of multiple cancer cells, including HeLa, DU145, H1975, and A549 cell lines. In addition, Sal A inhibited proliferation of DU145 cell lines stimulated by exogenous ET-1 treatment. Moreover, the cytotoxicity and cardio-toxicity of Sal A were assessed in human umbilical vein endothelial cells (HUVEC) and Human-induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs), which proved that Sal A demonstrates no cytotoxicity or cardiotoxicity. Collectively, our findings indicate that Sal A is a novel anti-cancer candidate through targeting ETAR. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266802]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhang, Qiao; Wang, Shifeng; Yu, Yangyang; Sun, Shengnan; Zhang, Yuxin; Zhang, Yanling; Yang, Wei; Li, Shiyou; Qiao, Yanjiang |
| 作者单位 | 1.Technical Department, ACEA Biosciences Inc., No. 5 Sandunxiyuan Road, Hangzhou 310030, China. paddy; 2.School of Chinese Materia Medica, Beijing University of Chinese Medicine, No. 6 Wangjingzhonghuan South Road, Chaoyang District, Beijing 100102, China; 3.Pharmacogenetics, HD Biosciences, Co., Ltd., 590 Ruiqing Road, Zhangjiang Hi-Tech Park East Campus, Pudong New Area, Shanghai 201201, China; 4.Beijing Institute of Genomics, Chinese Academy of Sciences, No. 1 Beichen West Road, Chaoyang District, Beijing 100101, China |
| 推荐引用方式 GB/T 7714 | Zhang, Qiao,Wang, Shifeng,Yu, Yangyang,et al. Salvianolic Acid A, as a Novel ETA Receptor Antagonist, Shows Inhibitory Effects on Tumor in Vitro[J]. International journal of molecular sciences,2016,17(8). |
| APA | Zhang, Qiao.,Wang, Shifeng.,Yu, Yangyang.,Sun, Shengnan.,Zhang, Yuxin.,...&Qiao, Yanjiang.(2016).Salvianolic Acid A, as a Novel ETA Receptor Antagonist, Shows Inhibitory Effects on Tumor in Vitro.International journal of molecular sciences,17(8). |
| MLA | Zhang, Qiao,et al."Salvianolic Acid A, as a Novel ETA Receptor Antagonist, Shows Inhibitory Effects on Tumor in Vitro".International journal of molecular sciences 17.8(2016). |
入库方式： OAI收割
来源：上海药物研究所
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