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一种新型苯并噻唑-2-硫醇衍生物在小鼠乳腺癌模型中的抗肿瘤和抗转移活性

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

作者信息

Hu XiaoLin, Li Sen, He Yan, Ai Ping, Wu Shaoyong, Su Yonglin, Li Xiaolin, Cai Lei, Peng Xingchen

机构信息

Department of Nursing, West China Hospital, Sichuan University, Chengdu, China.

Department of Spinal Surgery, Traditional Chinese Medicine Hospital of SouthWest Medical University, Luzhou, China.

出版信息

Oncotarget. 2017 Feb 14;8(7):11887-11895. doi: 10.18632/oncotarget.14431.

DOI:10.18632/oncotarget.14431
PMID:28060755
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5355312/
Abstract

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.

摘要

转移性乳腺癌的预后一直很差。因此，开发对转移性乳腺癌毒性较小的新型药物迫在眉睫。我们实验室设计并合成了一种源自苯并噻唑-2-硫醇的新药（XC-591）。在本研究中，我们试图评估XC-591治疗对4T1小鼠模型中原发性乳腺癌和肺转移的影响。此外，我们试图发现其可能的分子作用机制。MTT实验表明XC-591对多种癌细胞具有显著的抗癌活性。此外，通过集落形成试验，XC-591显著抑制了4T1细胞的增殖。体内结果显示，XC-591可抑制4T1模型中的生长和转移。此外，组织学分析表明，XC-591治疗可增加体内细胞凋亡、抑制增殖和血管生成。此外，在整个研究过程中，XC-591并未导致明显的药物相关毒性。分子机制表明，XC-591可抑制RhoGDI，激活caspase-3并降低磷酸化Akt。目前的数据对于进一步探索这种新型小分子抑制剂可能具有重要意义。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/b808b9bbcb0e/oncotarget-08-11887-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/45ad9844002a/oncotarget-08-11887-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/4f752c7ca40f/oncotarget-08-11887-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/b90cd94626d1/oncotarget-08-11887-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/98636c95dd14/oncotarget-08-11887-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/eb3598787779/oncotarget-08-11887-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/e93a62e7ce39/oncotarget-08-11887-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/b808b9bbcb0e/oncotarget-08-11887-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/45ad9844002a/oncotarget-08-11887-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/4f752c7ca40f/oncotarget-08-11887-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/b90cd94626d1/oncotarget-08-11887-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/98636c95dd14/oncotarget-08-11887-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/eb3598787779/oncotarget-08-11887-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/e93a62e7ce39/oncotarget-08-11887-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a208/5355312/b808b9bbcb0e/oncotarget-08-11887-g007.jpg

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