Cardiovascular Medicine Center, Affiliated Hospital of Guangdong Medical University, Zhanjiang 524001, China.
Laboratory of Cardiovascular Diseases, Guangdong Medical University, Zhanjiang 524001, China.
Biomed Res Int. 2017;2017:6147294. doi: 10.1155/2017/6147294. Epub 2017 Mar 27.
This study aimed to investigate the effects and mechanisms of quercetin on pulmonary arterial endothelial cell (PAEC) transdifferentiation into smooth muscle-like cells. TGF-1-induced PAEC transdifferentiation models were applied to evaluate the pharmacological actions of quercetin. PAEC proliferation was detected with CCK8 method and BurdU immunocytochemistry. Meanwhile, the identification and transdifferentiation of PAECs were determined by FVIII immunofluorescence staining and -SMA protein expression. The related mechanism was elucidated based on the levels of Akt and Erk1/2 signal pathways. As a result, quercetin effectively inhibited the TGF-1-induced proliferation and transdifferentiation of the PAECs and activation of Akt/Erk1/2 cascade in the cells. In conclusion, quercetin is demonstrated to be effective for pulmonary arterial hypertension (PAH) probably by inhibiting endothelial transdifferentiation possibly via modulating Akt and Erk1/2 expressions.
本研究旨在探讨槲皮素对肺动脉内皮细胞(PAEC)向平滑肌样细胞转化的作用及其机制。采用 TGF-β1 诱导的 PAEC 转化模型来评估槲皮素的药理作用。用 CCK8 法和 BrdU 免疫细胞化学法检测 PAEC 的增殖。同时,通过 FVIII 免疫荧光染色和 -SMA 蛋白表达来鉴定和检测 PAEC 的转化。基于 Akt 和 Erk1/2 信号通路的水平来阐明相关机制。结果表明,槲皮素能有效抑制 TGF-β1 诱导的 PAEC 增殖和转化以及细胞内 Akt/Erk1/2 级联的激活。综上所述,槲皮素可能通过调节 Akt 和 Erk1/2 的表达来抑制内皮细胞的转化,从而对肺动脉高压(PAH)有效。