Department of Oncology, Korea University Guro Hospital, 148 Gurodong-gil, Guro-gu, Seoul 152-703, Republic of Korea.
Department of Oncology, Korea University Guro Hospital, 148 Gurodong-gil, Guro-gu, Seoul 152-703, Republic of Korea; Graduate School of Medicine, Korea University College of Medicine, Seoul, Republic of Korea.
Food Chem Toxicol. 2018 Jun;116(Pt B):70-76. doi: 10.1016/j.fct.2018.04.005. Epub 2018 Apr 6.
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发挥重要作用。尽管栀子中的栀子苷已被证明具有抗肿瘤活性，但它在抑制 HIF-1 及其下游靶基因中的作用尚不清楚。我们使用结肠癌细胞系 HCT116 研究了栀子苷对 HIF-1α 细胞内水平和 VEGF 细胞外水平的影响。我们观察到栀子苷通过调节蛋白降解，抑制包括 HCT116 在内的各种癌细胞在缺氧下 HIF-1α 的积累。栀子苷还通过阻断细胞外信号调节激酶信号通路，抑制 VEGF 的表达和结肠癌细胞的侵袭。综上所述，我们的研究结果为栀子苷在抑制结肠癌进展中的潜在作用提供了新的见解。
