involvementofestrogenreceptorinfarrerolinhibitionofratthoracicaortavascularsmoothmusclecellproliferation

	involvementofestrogenreceptorinfarrerolinhibitionofratthoracicaortavascularsmoothmusclecellproliferation
	Li Qunyi 1; Chen Li 2; Zhu Yanhui 1; Zhang Meng 1; Wang Yiping 2; Wang Mingwei 1
刊名	actapharmacologicasinica
	2011
卷号	032 期号:004 页码:433
关键词	血管平滑肌雌激素受体细胞增殖主动脉大鼠细胞周期蛋白诱导培养 DNA合成
ISSN号	1671-4083
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 pmol/L） inhibited VSMC proliferation and DNA synthesis induced by 5% FBS in a concentration-dependent manner. The effects were associated with G1 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 μmol/L） induced 2.1-fold transcription of ER. In receptor binding assays, farrerol inhibited the binding of 3Hestradiol for ERα and ERβ with ICsovalues of 57 pmol/L and 2.7 μmol/L, respectively, implying that farrerol had a higher affinity for ERβ. Finally, the inhibition of VSMC proliferation by farrerol （3 μmol/L） was abolished by the specific ERβ antagonist PHTPP （5 μmol/L）. Conclusion： Farrerol acts as a functional phytoestrogen to inhibit FBS-induced VSMC proliferation, mainly via interaction with ERβ, which may be helpful in the treatment of cardiovascular diseases related to abnormal VSMCs proliferation.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/286005]
专题	中国科学院上海药物研究所
作者单位	1.中国科学院 2.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	Li Qunyi,Chen Li,Zhu Yanhui,et al. involvementofestrogenreceptorinfarrerolinhibitionofratthoracicaortavascularsmoothmusclecellproliferation[J]. actapharmacologicasinica,2011,032(004):433.
APA	Li Qunyi,Chen Li,Zhu Yanhui,Zhang Meng,Wang Yiping,&Wang Mingwei.(2011).involvementofestrogenreceptorinfarrerolinhibitionofratthoracicaortavascularsmoothmusclecellproliferation.actapharmacologicasinica,032(004),433.
MLA	Li Qunyi,et al."involvementofestrogenreceptorinfarrerolinhibitionofratthoracicaortavascularsmoothmusclecellproliferation".actapharmacologicasinica 032.004(2011):433.