Effects of diphyllin as a novel V-ATPase inhibitor on TE-1 and ECA-109 cells

Chen,Haijiao; Liu,Pengfei; Zhang,Ting; Gao,Yi; Zhang,Yingdi; Shen,Xiuyun; Li,Xiao; Shen,Weidong

doi:10.3892/or.2018.6191

Effects of diphyllin as a novel V-ATPase inhibitor on TE-1 and ECA-109 cells

Authors:
- Haijiao Chen
- Pengfei Liu
- Ting Zhang
- Yi Gao
- Yingdi Zhang
- Xiuyun Shen
- Xiao Li
- Weidong Shen
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Affiliations: Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, Jiangsu 221000, P.R. China
Published online on: January 4, 2018 https://doi.org/10.3892/or.2018.6191
Pages: 921-928
Copyright: © Chen et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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Abstract

Diphyllin is a natural component of traditional Chinese medicine, which effectively inhibits V-ATPase activity and affects the progression of cancer. However, few studies have been conducted on esophageal cancer, and the mechanisms remain to be elucidated. The present study revealedthat diphyllin inhibited proliferation and induced S arrest in esophageal cancer cell lines TE-1 and ECA-109. Further experiments revealed that diphyllin inhibited V-ATPase activity and decreased the mRNA expression of mammalian target of rapamycin complex 1 (mTORC1), hypoxia-inducible factor-1α (HIF-1α), and vascular endothelial growth factor (VEGF). The present study also revealed that diphyllin inhibited proliferation and reduced the formation of new blood vessels. Diphyllin inhibited blood metastasis by regulating the mTORC1/HIF-1α-/VEGF pathway, therefore it could be considered as a new V-ATPase inhibitor to treat esophageal cancer.

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