2. Academic Validation
  3. Angoline: a selective IL-6/STAT3 signaling pathway inhibitor isolated from Zanthoxylum nitidum

Angoline: a selective IL-6/STAT3 signaling pathway inhibitor isolated from Zanthoxylum nitidum

  • Phytomedicine. 2014 Jul-Aug;21(8-9):1088-91. doi: 10.1016/j.phymed.2014.04.001.
Jiawei Liu 1,  Qing Zhang 2,  Yushan Ye 3,  Wuguo Li 3,  Junxin Qiu 3,  Jingli Liu 2,  Ruoting Zhan 3,  Weiwen Chen 3,  Qiang Yu 2
Affiliations

Affiliations

  • 1 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. Electronic address: [email protected].
  • 2 Department of Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, People's Republic of China.
  • 3 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.
PMID: 24863036 DOI: 10.1016/j.phymed.2014.04.001
Abstract

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.

Keywords

Angoline; Inhibitor; STAT3 signaling pathway; Zanthoxylum nitidum.

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