安哥林：一种从两面针中分离出的选择性白细胞介素-6/信号转导和转录激活因子3信号通路抑制剂。
Angoline: a selective IL-6/STAT3 signaling pathway inhibitor isolated from Zanthoxylum nitidum.
作者信息
Liu Jiawei, Zhang Qing, Ye Yushan, Li Wuguo, Qiu Junxin, Liu Jingli, Zhan Ruoting, Chen Weiwen, Yu Qiang
机构信息
Ministry of Education Key Laboratory of Chinese Medicinal Plants Resource from Lingnan, Research Center of Medicinal Plants Resource Science and Engineering, Guangzhou University of Chinese Medicine, Guangzhou, People's Republic of China.
Department of Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, People's Republic of China.
出版信息
Phytomedicine. 2014 Jul-Aug;21(8-9):1088-91. doi: 10.1016/j.phymed.2014.04.001. Epub 2014 May 24.
STAT3 signaling pathway is an important target for human cancer therapy. Thus, the identification of small-molecules that target STAT3 signaling will be of great interests in the development of anticancer agents. The aim of this study was to identify novel inhibitors of STAT3 pathway from the roots of Zanthoxylum nitidum (Roxb.) DC. The bioassay-guided fractionation of MeOH extract of Z. nitidum using a STAT3-responsive gene reporter assay led to the isolation of angoline (1) as a potent and selective inhibitor of the STAT3 signaling pathway (IC50=11.56 μM). Angoline inhibited STAT3 phosphorylation and its target gene expression and consequently induced growth inhibition of human cancer cells with constitutively activated STAT3 (IC50=3.14-4.72 μM). This work provided a novel lead for the development of anti-cancer agents targeting the STAT3 signaling pathway.
信号转导与转录激活因子3（STAT3）信号通路是人类癌症治疗的重要靶点。因此，鉴定靶向STAT3信号的小分子对于抗癌药物的开发具有重要意义。本研究旨在从两面针（Zanthoxylum nitidum (Roxb.) DC.）的根中鉴定STAT3信号通路的新型抑制剂。利用STAT3反应基因报告试验对两面针甲醇提取物进行生物活性导向分离，得到了安吉洛宁（1），它是一种有效的、选择性的STAT3信号通路抑制剂（IC50 = 11.56 μM）。安吉洛宁抑制STAT3磷酸化及其靶基因表达，从而诱导具有组成性激活STAT3的人类癌细胞生长抑制（IC50 = 3.14 - 4.72 μM）。这项工作为开发靶向STAT3信号通路的抗癌药物提供了新的先导化合物。
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