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硝呋太尔,一种对人胃癌细胞具有强大活性的新型信号转导和转录激活因子3(STAT3)抑制剂。

Nifuratel, a novel STAT3 inhibitor with potent activity against human gastric cancer cells.

作者信息

Zheng Hailun, Hong Huang, Zhang Lulu, Cai Xiong, Hu Meng, Cai Yuepiao, Zhou Bin, Lin Jiayuh, Zhao Chengguang, Hu Wanle

机构信息

Department of Coloproctology, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University.

Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, Zhejiang, People's Republic of China.

出版信息

Cancer Manag Res. 2017 Nov 1;9:565-572. doi: 10.2147/CMAR.S146173. eCollection 2017.

Abstract

Activation of the signal transducer and activator of transcription 3 (STAT3) is observed in multiple cancer types, including gastric cancer, and represents a potential drug target for chemotherapy. Currently, clinically available small-molecule inhibitors targeting STAT3 are lacking. Here, we report that nifuratel, an antiprotozoal and antifungal drug, is a potent inhibitor of STAT3. We found that nifuratel significantly suppressed proliferation and induced apoptosis of gastric cancer cells. Studies of the mechanism of action of nifuratel indicated that it acts by inhibiting the constitutive and interleukin-6-induced STAT3 activation. Taken together, our findings demonstrate that nifuratel may be a novel, clinically accessible STAT3 inhibitor in gastric cancer cells.

摘要

在包括胃癌在内的多种癌症类型中都观察到信号转导和转录激活因子3(STAT3)的激活,这代表了化疗的一个潜在药物靶点。目前,临床上缺乏针对STAT3的小分子抑制剂。在此,我们报告硝呋太尔,一种抗原生动物和抗真菌药物,是一种有效的STAT3抑制剂。我们发现硝呋太尔显著抑制胃癌细胞的增殖并诱导其凋亡。对硝呋太尔作用机制的研究表明,它通过抑制组成型和白细胞介素-6诱导的STAT3激活来发挥作用。综上所述,我们的研究结果表明硝呋太尔可能是一种新型的、临床上可获得的胃癌细胞STAT3抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8624/5677376/aafd431f9d4d/cmar-9-565Fig1.jpg

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