Department of Pathophysiology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, Henan 450001, P.R. China.
Oncol Rep. 2018 Jun;39(6):2942-2950. doi: 10.3892/or.2018.6390. Epub 2018 Apr 23.
Eupatilin, a type of flavonoid compound, has potential anti‑inflammatory and antitumor roles in gastric cancer and endometrial cancer; however, the effect of eupatilin on human esophageal cancer and the underlying molecular mechanisms remain unclear. In the present study, we investigated the antitumor effect of eupatilin on human esophageal cancer cells in vitro and in vivo. We found that eupatilin inhibited the proliferation and colony formation of esophageal cancer TE1 cells. DNA content analysis showed that eupatilin induced cell cycle arrest of TE1 cells at the G0/G1 phase. In addition, our results suggested that eupatilin suppressed TE1 cell proliferation by targeting the Akt/GSK3β and MAPK/ERK signaling cascades. Furthermore, treatment with eupatilin was found to decrease tumor volume in a TE1 xenograft mouse model, and the phosphorylation of Akt and ERK1/2 was inhibited by eupatilin in the tumor tissue. Notably, no obvious weight loss for the mice was detected. In conclusion, the present results indicate that the antiproliferative effect of eupatilin on esophageal cancer TE1 cells is associated with inhibition of the Akt and ERK pathways.
柚皮素是一种黄酮类化合物，在胃癌和子宫内膜癌中具有潜在的抗炎和抗肿瘤作用；然而，柚皮素对人食管癌的作用及其潜在的分子机制尚不清楚。在本研究中，我们研究了柚皮素在体外和体内对人食管癌细胞的抗肿瘤作用。我们发现柚皮素抑制食管癌 TE1 细胞的增殖和集落形成。DNA 含量分析表明，柚皮素诱导 TE1 细胞在 G0/G1 期停滞。此外，我们的结果表明，柚皮素通过靶向 Akt/GSK3β 和 MAPK/ERK 信号通路抑制 TE1 细胞增殖。此外，柚皮素治疗可降低 TE1 异种移植小鼠模型中的肿瘤体积，柚皮素可抑制肿瘤组织中 Akt 和 ERK1/2 的磷酸化。值得注意的是，未观察到小鼠明显的体重减轻。总之，本研究结果表明，柚皮素对食管癌 TE1 细胞的增殖抑制作用与抑制 Akt 和 ERK 通路有关。
