Neoplasma. 2016;63(3):351-61. doi: 10.4149/303_150723N405.
Epithelial-mesenchymal transition (EMT) is considered as the most important mechanism that underlies the initiation of cancer metastasis. Here we report that Physicon 8-O-β-glucopyranoside (PG), a major active ingredient from a traditional Chinese herbal medicine Rumex japonicus Houtt, is capable of preventing human colorectal cancer cells from hypoxia-induced EMT. The treatment of the cells with PG reversed the EMT-related phenotype that has the morphological changes, down-regulation of E-cadherin, and hypoxia-induced cell migration and invasion. The effect was mediated at least in part by inhibiting the mRNA and protein expressions of EMMPRIN via modulation of PTEN/Akt/HIF-1α pathway. In addition, we found that PG-mediated prevention of EMT involved blockade of the hypoxia-induced up-regulation of Snail, Slug and Twist. In summary, this study showed that PG can prevent EMT induced by hypoxia, the environment that commonly exists in the center of a solid tumor. Given the low toxicity of PG to the healthy tissues, our study suggests that PG can serve as a safe therapeutic agent for suppressing cancer metastasis.
上皮-间充质转化（EMT）被认为是癌症转移起始的最重要机制。在这里，我们报告 Physicon 8-O-β-吡喃葡萄糖苷（PG），一种来自传统中药虎杖的主要活性成分，能够防止人结直肠癌细胞缺氧诱导的 EMT。用 PG 处理细胞可逆转 EMT 相关表型，包括形态变化、E-钙黏蛋白下调以及缺氧诱导的细胞迁移和侵袭。该作用至少部分通过调节 PTEN/Akt/HIF-1α 通路抑制 EMMPRIN 的 mRNA 和蛋白表达来介导。此外，我们发现 PG 介导的 EMT 预防涉及阻断缺氧诱导的 Snail、Slug 和 Twist 的上调。总之，这项研究表明 PG 可以预防 EMT 诱导的缺氧，这是实体瘤中心常见的环境。鉴于 PG 对健康组织的低毒性，我们的研究表明 PG 可作为抑制癌症转移的安全治疗剂。
