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Antitumor and antimetastatic activities of a novel benzothiazole-2-thiol derivative in a murine model of breast cancer.

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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

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关键词： benzothiazole-2-thiol derivative breast cancer proliferation metastasis apoptosis

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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.

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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

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第一作者机构： [1]Department of Nursing, West China Hospital, Sichuan University, Chengdu, China

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