机构：[1]Department of Nursing, West China Hospital, Sichuan University, Chengdu, China[2]Department of Spinal Surgery, Traditional Chinese Medicine Hospital of SouthWest Medical University, Luzhou, China[3]Department of Medical Oncology, Cancer Center, State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, China[4]Department of Rehabilitation, West China Hospital, Sichuan University, Chengdu, China[5]Department of Pathophysiology, Basic Medical College, Jilin University, Changchun, China[6]Hepatobiliary Surgery Institute, Southwest Hospital, Third Military Medical University, Chongqing, China
The prognosis of metastatic breast cancer is always very poor. Thus, it is urgent to develop novel drugs with less toxicity against metastatic breast cancer. A new drug (XC-591) derived from benzothiazole-2-thiol was designed and synthesized in our lab. In this study, we tried to assess effects of XC-591 treatment on primary breast cancer and pulmonary metastasis in 4T1 mice model. Furthermore, we tried to discover its possible molecular mechanism of action. MTT experiment showed XC-591 had significant anti-cancer activity on diverse cancer cells. Furthermore, XC-591 significantly suppressed the proliferation of 4T1 cells by colony formation assay. The in vivo results displayed that XC-591 could inhibit the growth and metastasis in 4T1 model. Moreover, histological analysis revealed that XC-591 treatment increased apoptosis, inhibited proliferation and angiogenesis in vivo. In addition, XC-591 did not contribute to obvious drug associated toxicity during the whole study. Molecular mechanism showed XC-591 could inhibit RhoGDI, activate caspase-3 and decrease phosphorylated Akt. The present data may be important to further explore this kind of new small-molecule inhibitor.
基金：
National Natural Sciences Foundation of ChinaNational Natural Science Foundation of China [81402494, 81672386]; Science and technology support program of sichuan province [2015SZ0076, 2014HH0063]; international visiting program for excellent young scholars of SCU
语种：
外文
WOS：
PubmedID：
中科院(CAS)分区：
出版当年[2017]版：
大类|2 区医学
小类|2 区肿瘤学3 区细胞生物学
最新[2023]版：
无
第一作者：
第一作者机构：[1]Department of Nursing, West China Hospital, Sichuan University, Chengdu, China
共同第一作者：
通讯作者：
通讯机构：[3]Department of Medical Oncology, Cancer Center, State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, China
推荐引用方式(GB/T 7714)：
XiaoLin Hu,Sen Li,Yan He,et al.Antitumor and antimetastatic activities of a novel benzothiazole-2-thiol derivative in a murine model of breast cancer.[J].Oncotarget.2017,8(7):11887-11895.doi:10.18632/oncotarget.14431.
APA：
XiaoLin Hu,Sen Li,Yan He,Ping Ai,Shaoyong Wu...&Xingchen Peng.(2017).Antitumor and antimetastatic activities of a novel benzothiazole-2-thiol derivative in a murine model of breast cancer..Oncotarget,8,(7)
MLA：
XiaoLin Hu,et al."Antitumor and antimetastatic activities of a novel benzothiazole-2-thiol derivative in a murine model of breast cancer.".Oncotarget 8..7(2017):11887-11895
