Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, Jiangsu 221000, P.R. China.
Oncol Rep. 2018 Mar;39(3):921-928. doi: 10.3892/or.2018.6191. Epub 2018 Jan 4.
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.
二氢菲是一种中药的天然成分，能有效抑制 V-ATPase 活性，影响癌症的进展。然而，目前针对食管癌的研究较少，其机制尚不清楚。本研究表明，二氢菲可抑制食管癌细胞系 TE-1 和 ECA-109 的增殖并诱导 S 期停滞。进一步的实验表明，二氢菲可抑制 V-ATPase 活性，降低哺乳动物雷帕霉素靶蛋白复合物 1（mTORC1）、缺氧诱导因子-1α（HIF-1α）和血管内皮生长因子（VEGF）的 mRNA 表达。本研究还表明，二氢菲可抑制增殖并减少新血管的形成。二氢菲通过调节 mTORC1/HIF-1α-/VEGF 通路抑制血转移，因此它可以被认为是一种治疗食管癌的新型 V-ATPase 抑制剂。
