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.

STAT3信号通路是人类癌症治疗的重要目标。因此，鉴定靶向STAT3信号转导的小分子将在抗癌剂的开发中引起极大兴趣。这项研究的目的是从花椒（Roxb。）DC的根部确定STAT3途径的新型抑制剂。的甲醇提取物的生物测定引导的分级分离Z.两面针使用导致angoline（的隔离STAT3应答基因报告基因分析1）作为STAT3信号传导途径的有效的和选择性的抑制剂（IC ₅₀  = 11.56μM）。Anggoline抑制STAT3磷酸化及其靶基因的表达，并因此诱导组成型激活STAT3（IC₅₀  = 3.14–4.72μM）。这项工作为靶向STAT3信号通路的抗癌药的开发提供了新的线索。