Cryptotanshinone inhibits proliferation and induces apoptosis of breast cancer MCF-7 cells via GPER mediated PI3K/AKT signaling pathway

被引:13
|
作者
Shi, Danning [1 ]
Li, Hongbo [2 ]
Zhang, Zeye [1 ]
He, Yueshuang [1 ]
Chen, Meng [3 ]
Sun, Liping [1 ]
Zhao, Piwen [1 ]
机构
[1] Beijing Univ Chinese Med, Sch Life Sci, Beijing 100029, Peoples R China
[2] Shaanxi Univ Chinese Med, Affiliated Hosp, Dept Gynecol, Shaanxi 712000, Peoples R China
[3] Beijing Univ Chinese Med, Sch Tradit Chinese Med, Beijing 100029, Peoples R China
来源
PLOS ONE | 2022年 / 17卷 / 01期
基金
中国国家自然科学基金;
关键词
GROWTH; CHINA; RESISTANCE; SURVIVAL;
D O I
10.1371/journal.pone.0262389
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
G protein-coupled estrogen receptor (GPER) was reported to be a potential target in the breast cancer therapy. This study aimed to illuminate the function of GPER and its mediated PI3K/AKT pathway in cryptotanshinone (CPT) inducing cell apoptosis and antiproliferation effect on GPER positive breast cancer MCF-7 cells. Cell proliferation was tested by MTT assay. Apoptosis rates were tested by Annexin V-FITC/PI double staining and the cell cycle was researched by flow cytometry. Autodock vina was applied to make molecular docking between CPT or estradiol and GPER. siRNA technique and GPER specific agonist G-1 or antagonist G-15 were applied to verify the mediated function of GPER. Apoptosis and cell cycle related proteins, as well as the key proteins on PI3K/AKT signaling pathway were detected by western blot. The results indicated that CPT could exert antiproliferation effects by arresting cell cycle in G2/M phase and downregulating the expression of cyclin D, cyclin B and cyclin A. Besides, apoptosis induced by CPT was observed. CPT might be a novel GPER binding compounds. Significantly, suppression of PI3K/AKT signal transduction by CPT was further increased by G-1 and decreased by G-15. The study revealed that the effect of antiproliferation and apoptosis treating with CPT on MCF-7 cells might be through the downregulation of PI3K/AKT pathway mediated by activated GPER.
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页数:14
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