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Osthole inhibits the migration and invasion of highly metastatic breast cancer cells by suppressing ITGα3/ ITGβ5 signaling

Yue-qiang Chen1, Hai-yan Song2, Zhong-yan Zhou1, Jiao Ma1, Zhan-yang Luo1, Ying Zhou3, Jian-yi Wang4, Sheng Liu1, Xiang-hui Han1
1 Institute of Chinese Traditional Surgery, Longhua Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 200032, China
2 Institute of Digestive Diseases, Longhua Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 200032, China
3 Shanghai TCM-integrated Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 200082, China
4 Department of Liver Disease, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
Correspondence to: Jian-yi Wang: wjydyj@163.com, Sheng Liu: lshtcm@126.com, Xiang-hui Han: hanxianghui1106@163.com,
DOI: 10.1038/s41401-021-00757-7
Received: 1 April 2021
Accepted: 2 August 2021
Advance online: 23 August 2021

Abstract

Metastasis is the leading cause of death in breast cancer patients. Osthole, as an active compound detected in the traditional Chinese medicine Wenshen Zhuanggu Formula, has shown a promising anti-metastatic activity in human breast cancer cells, but the underlying mechanisms remain ambiguous. In this study we elucidated the anti-metastatic mechanisms of osthole in highly metastatic breast cancer cells and a zebrafish xenograft model. We showed that the expression of integrin α3 (ITGα3) and integrin β5 (ITGβ5) was upregulated in highly metastatic MDA-MB-231, MDA-MB-231BO breast cancer cell lines but was downregulated in poorly metastatic MCF-7 breast cancer cell line, which might be the key targets of osthole’s anti-metastatic action. Furthermore, we showed that knockdown of ITGα3 and ITGβ5 attenuated breast cancer cell migration and invasion possibly via suppression of FAK/ Src/Rac1 pathway, whereas overexpression of ITGα3 and ITGβ5 caused the opposite effects. Consistently, osthole significantly inhibited breast cancer metastasis by downregulating ITGα3/ITGβ5 signaling in vitro and in vivo. These results provide new evidence that osthole may be developed as a candidate therapeutic drug for metastatic breast cancer.
Keywords: osthole; Wenshen Zhuanggu Formula; breast cancer; metastasis; ITGα3; ITGβ5; FAK/Src/Rac1 pathway

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