Impact Factor 3.845 | CiteScore 3.92
More on impact ›

Original Research ARTICLE Provisionally accepted The full-text will be published soon. Notify me

Front. Pharmacol. | doi: 10.3389/fphar.2019.01248

Eupafolin Suppresses Esophagus Cancer Growth by Targeting TOPK Protein Kinase

 Xiaoming Fan1*, Juanyan Tao2,  Mangaladoss Fredimoses3, Zhihui Jiang1, Jilei Ma4, Shude Li5, Kunpeng Zhang1 and Xiaoying Zhang6
  • 1Henan Joint International Research Laboratory of Veterinary Biologics Research and Application, Anyang Institute of Technology, China
  • 2Environmental Safety and Human Health, Wenzhou Medical University, China
  • 3China-US (Henan) Hormel Cancer Institute, China
  • 4Clinical Laboratory, First Affiliated Hospital of Zhengzhou University, China
  • 5Biochemistry and Molecular Biology, Kunming Medical University, China
  • 6Henan Joint International Research Laboratory of Veterinary Biologics Research and Application, Northwest A&F University, China

Abstract
Eupafolin is the main bioactive component extracted from the traditional Chinese medicine Ay Tsao (Artemisia vulgaris L.), and its anti-tumor activity have had been studied in previous researches. T-LAK cell-originated protein kinase (TOPK) belongs to serine/threonine protein kinase, is highly expressed in several cancer cells and tissues, such as colon cancer, lung cancer, esophagus cancer and so on. Therefore, it was recognized as an important target for treating tumors. Nowadays, we found that Eupafolin suppressed TOPK activities at the first time in vitro and in vivo. The cells study indicated that Eupafolin suppressed TOPK activities in JB6 Cl41 and KYSE450 cells. Furthermore, knockdown of TOPK in KYSE450 cells decreased their sensitivities to Eupafolin. The animal study showed that the injection of Eupafolin in patient-derived xenograft (PDX) mouse effectively suppressed tumor growth. Histone H3 and Ki67 were reduced and cleaved caspase 3 was increased in tumor tissues after Eupafolin treatment. To sum up, Eupafolin as an TOPK inhibitor can suppress growth of esophagus cancer in vitro and in vivo. The TOPK downstream signaling molecule Histone H3 in tumor tissues was also reduced after Eupafolin treatment. In short, Eupafolin can suppress growth of esophagus cancer cells as an TOPK inhibitor both in vitro and in vivo.

Keywords: Eupafolin, esophagus cancer, TOPK (T-LAK cell-originated protein kinase);, inhibitor, Artemisia

Received: 11 Jun 2019; Accepted: 27 Sep 2019.

Copyright: © 2019 Fan, Tao, Fredimoses, Jiang, Ma, Li, Zhang and Zhang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

* Correspondence: Mx. Xiaoming Fan, Anyang Institute of Technology, Henan Joint International Research Laboratory of Veterinary Biologics Research and Application, Anyang, China, fanxiaom1987@163.com