Involvement of estrogen receptor-beta in farrerol inhibition of rat thoracic aorta vascular smooth muscle cell proliferation
文献类型：期刊论文
| 作者 | Li, Qun-yi2; Chen, Li1; Zhu, Yan-hui2; Zhang, Meng2; Wang, Yi-ping1 ; Wang, Ming-wei1,2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2011-04 |
| 卷号 | 32期号:4页码:433-440 |
| 关键词 | farrerol phytoestrogen estrogen receptor vascular smooth muscle cells cell proliferation cell cycle ERK1/2 receptor binding assay |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2011.1 |
| 文献子类 | Article |
| 英文摘要 | Aim: To investigate the effect of farrerol, a major active component isolated from a traditional Chinese herb "Man-shan-hong" (the dried leaves of Rhododendron dauricum L) on fetal bovine serum (FBS)-induced proliferation of cultured vascular smooth muscle cells (VSMCs) of rat thoracic aorta. Methods: VSMCs proliferation, DNA synthesis and cell cycle progression were studied using the MTT assay, bromodeoxyuridine (BrdU) incorporation and flow cytometry, respectively. The mRNA levels of cell cycle proteins were quantified using real-time RT-PCR, and the phosphorylation of ERK1/2 was determined using Western blotting. Reporter gene and receptor binding assays were employed to study the interaction between farrerol and estrogen receptors (ERs). Results: Farrerol (0.3-10 mu mol/L) inhibited VSMC proliferation and DNA synthesis induced by 5% FBS in a concentration-dependent manner. The effects were associated with G(1) cell cycle arrest, down-regulation of cell cycle proteins and reduction in FBS-induced ERK1/2 phosphorylation. Using a reporter gene, it was found that farrerol (3 mu mol/L) induced 2.1-fold transcription of ER. In receptor binding assays, farrerol inhibited the binding of [H-3] estradiol for ER alpha and ER beta with IC50 values of 57 mu mol/L and 2.7 mu mol/L, respectively, implying that farrerol had a higher affinity for ER beta. Finally, the inhibition of VSMC proliferation by farrerol (3 mu mol/L) was abolished by the specific ER beta antagonist PHTPP (5 mu mol/L). Conclusion: Farrerol acts as a functional phytoestrogen to inhibit FBS-induced VSMC proliferation, mainly via interaction with ER beta, which may be helpful in the treatment of cardiovascular diseases related to abnormal VSMCs proliferation. |
| WOS关键词 | ACTIVATED PROTEIN-KINASE ; RANDOMIZED CONTROLLED-TRIAL ; RHODODENDRON-DAURICUM L. ; POSTMENOPAUSAL WOMEN ; CAPILLARY-ELECTROPHORESIS ; ELECTROCHEMICAL DETECTION ; CARDIOVASCULAR-DISEASE ; INJURY RESPONSE ; RISK-FACTORS ; HEALTH |
| 资助项目 | Ministry of Science and Technology of China[2009ZX09302-001] ; Shanghai Municipality Government[08DZ2291300] ; Shanghai Municipality government[09DZ2291200] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4178085 |
| WOS记录号 | WOS:000289194200004 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278569]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Wang, Ming-wei |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab New Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Li, Qun-yi,Chen, Li,Zhu, Yan-hui,et al. Involvement of estrogen receptor-beta in farrerol inhibition of rat thoracic aorta vascular smooth muscle cell proliferation[J]. ACTA PHARMACOLOGICA SINICA,2011,32(4):433-440. |
| APA | Li, Qun-yi,Chen, Li,Zhu, Yan-hui,Zhang, Meng,Wang, Yi-ping,&Wang, Ming-wei.(2011).Involvement of estrogen receptor-beta in farrerol inhibition of rat thoracic aorta vascular smooth muscle cell proliferation.ACTA PHARMACOLOGICA SINICA,32(4),433-440. |
| MLA | Li, Qun-yi,et al."Involvement of estrogen receptor-beta in farrerol inhibition of rat thoracic aorta vascular smooth muscle cell proliferation".ACTA PHARMACOLOGICA SINICA 32.4(2011):433-440. |
入库方式： OAI收割
来源：上海药物研究所
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