Cancer Metastasis Alert and Prevention Center, and Biopharmaceutical Photocatalysis, State Key Laboratory of Photocatalysis on Energy and Environment, Fuzhou University, Fuzhou 350002, China.
Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention, Fuzhou University, Fuzhou, China.
Sci Rep. 2016 Aug 2;6:30549. doi: 10.1038/srep30549.
We recently defined cancer metastatic chemoprevention as utilizing safe and effective molecules to comprehensively prevent the spark of activation-adhesion-extravasation-proliferation metastatic cascade caused by circulating tumor cells (CTCs). The strategy focuses on preventing the most important starting point of the cascade. We identified an extract from a well-known medical plant Murraya paniculata, which inhibited both embryonic implantation to human endometrium as traditionally-used for abortion and CTC adhesion to human endothelium. Here, we separated and characterized five coumarin-containing components (Z1-Z5) from the botanic extract. Flow cytometry revealed that within 1-100 μg/mL, Z3 and Z5 down-regulated EpCAM expression in human colon HCT116, whereas, Z1 and Z2 did oppositely. Warfarin and Z1-Z5 component mixture (CM) also down-regulated EpCAM expression. The down-regulation of EpCAM by Z3, Z5, CM and warfarin was confirmed by western blotting, and caused inhibition on adhesion of cancer cells to human endothelial cells. Rat coagulation study showed that warfarin prolonged prothrombin time, whereas, Z3 did not. The present studies revealed that, for the first time, warfarin and coumarin-like components Z3, Z5 and CM from Murraya paniculata could directly inhibit EpCAM-mediated cell-cell adhesion.
我们最近将癌症转移化学预防定义为利用安全有效的分子全面预防循环肿瘤细胞(CTCs)引起的激活-黏附-渗出-增殖转移级联反应的启动。该策略侧重于预防级联反应的最重要起点。我们从一种著名的药用植物九里香中鉴定出一种提取物,它既能抑制胚胎着床到人类子宫内膜(传统上用于堕胎),又能抑制 CTC 黏附到人类内皮细胞。在这里,我们从植物提取物中分离和鉴定了五种含香豆素的成分(Z1-Z5)。流式细胞术显示,在 1-100μg/mL 范围内,Z3 和 Z5 下调了人结肠 HCT116 中 EpCAM 的表达,而 Z1 和 Z2 则相反。华法林和 Z1-Z5 成分混合物(CM)也下调了 EpCAM 的表达。Z3、Z5、CM 和华法林下调 EpCAM 的作用通过 Western blot 得到证实,并抑制了癌细胞与内皮细胞的黏附。大鼠凝血研究表明,华法林延长了凝血酶原时间,而 Z3 则没有。本研究首次揭示,华法林和来自九里香的香豆素样成分 Z3、Z5 和 CM 可直接抑制 EpCAM 介导的细胞间黏附。