Hypoxia-inducible factor-1 (HIF-1) and vascular endothelial growth factor (VEGF) play important roles in cancer progression in various cancer cell lines. Although genipin, a constituent of Gardenia fruit, has been shown to have anti-tumor activity, its role in the suppression of HIF-1 and its downstream target genes is not well understood. We examined the effect of genipin on the intracellular level of HIF-1α and extracellular level of VEGF using the colon cancer cell line HCT116. We observed that genipin suppressed the accumulation of HIF-1α under hypoxia in various cancer cell lines, including HCT116, via the modulation of protein degradation. Genipin also suppressed the expression of VEGF and the invasion of colon cancer cells by blocking the extracellular signal-regulated kinase signaling pathway. Taken together, our results provide new insights into the potential role of genipin in suppressing colon cancer progression.

缺氧诱导因子1（HIF-1）和血管内皮生长因子（VEGF）在各种癌细胞系的癌症进展中起着重要作用。尽管Genipin是Garden子果实的一种成分，但已显示具有抗肿瘤活性，但其在抑制HIF-1及其下游靶基因中的作用尚未得到很好的了解。我们使用结肠癌细胞系HCT116检查了Genipin对HIF-1α的细胞内水平和VEGF的细胞外水平的影响。我们观察到，genipin通过调节蛋白质降解，抑制了缺氧条件下HIF-1α在包括HCT116在内的各种癌细胞系中的积累。Genipin还通过阻断细胞外信号调节激酶信号传导途径来抑制VEGF的表达和结肠癌细胞的侵袭。在一起