Emodin suppresses growth and invasion of colorectal cancer cells by inhibiting VEGFR2

被引：43

作者：

Dai, Guoliang ^{[1
]}

Ding, Kang ^{[2
]}

Cao, Qianyu ^{[3
]}

Xu, Tian ^{[1
]}

He, Fan ^{[1
]}

Liu, Shijia ^{[1
]}

Ju, Wenzheng ^{[1
]}

机构：

[1] Nanjing Univ Chinese Med, Affiliated Hosp, 155 Hanzhong Rd, Nanjing 210029, Jiangsu, Peoples R China

[2] Nanjing Univ Chinese Med, Affiliated Hosp 3, Jiangsu Integrate Colorectal Oncol Ctr, Natl Ctr Colorectal Surg, Nanjing 210001, Jiangsu, Peoples R China

[3] Nanjing Univ Chinese Med, Clin Coll 1, Nanjing 210023, Jiangsu, Peoples R China

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 2019年 / 859卷

基金：

中国国家自然科学基金;

关键词：

Emodin; VEGFR2; Colorectal cancer; HCT116; cell; Molecular docking; SIGNALING PATHWAY; EXPRESSION;

D O I：

10.1016/j.ejphar.2019.172525

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Emodin can effectively inhibit colorectal cancer cells, but the mechanism remains elusive. This study analyzed the changes of VEGFR2 signaling pathways in patients with colorectal cancer and the effects of emodin on HCT116 cells and xenograft tumor model. The expression levels of VEGFR2, PI3K, and p-AKT in colorectal cancer tissue samples were significantly higher than those in adjacent normal ones. Docking simulation confirmed that emodin bound the hydrophobic pocket and partially overlapped with the binding sites of VEGFR2, thus disrupting VEGFR2 dimerization. Western blotting further confirmed that emodin significantly inhibited the expression of VEGFR2, and reduced the expressions of PI3K and p-AKT in HCT116 cells. Furthermore, it suppressed the growth, adhesion and migration of HCT116 cells. In addition, emodin inhibited the tumor growth in xenograft model and the expressions of VEGFR2, PI3K and p-AKT in vivo. In conclusion, emodin suppressed the growth of colorectal cancer cells by inhibiting VEGFR2, as a potential candidate for therapy.

引用

页数：7

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