Hardwick James C H, van Santen Marije, van den Brink Gijs R, van Deventer Sander J H, Peppelenbosch Maikel P
Department of Experimental Internal Medicine, Academic Medical Center, Meibergdreef 9, 1105 AZ, Amsterdam, The Netherlands.
Carcinogenesis. 2004 Jul;25(7):1293-8. doi: 10.1093/carcin/bgh118. Epub 2004 Feb 19.
Aspirin and other non-steroidal anti-inflammatory drugs show efficacy in the prevention of colon cancer. The mechanism by which they do this is unclear. We used a commercially available DNA microarray to study changes in gene expression in 1176 cancer related genes in the HT29 colon cancer cell line induced by aspirin. Overall we find more genes that are significantly induced than are repressed. The pattern of gene expression changes is different at high concentrations of aspirin (5 mM) than at lower levels (500 and 50 microM). Genes involved in DNA damage signaling, nucleotide metabolism and the stress response are induced, and cell cycle related genes repressed. The small GTPase Rac1 is highly induced and this was confirmed by immunoblotting. We show using immunohistochemistry that Rac1 is expressed in mature colonocytes at the intercrypt table in human and mouse colon tissue. These results support the previous findings that aspirin has different actions at high concentrations than at low concentrations and further show the use of DNA array technology in the investigation of drug mechanisms of action. Furthermore, they point towards a role for Rac1 in the action of aspirin in colon cancer.
阿司匹林及其他非甾体抗炎药在预防结肠癌方面显示出疗效。其作用机制尚不清楚。我们使用一种市售的DNA微阵列来研究阿司匹林诱导的HT29结肠癌细胞系中1176个癌症相关基因的基因表达变化。总体而言,我们发现显著上调的基因比下调的基因更多。高浓度阿司匹林(5 mM)与低浓度(500和50 microM)时基因表达变化模式不同。参与DNA损伤信号传导、核苷酸代谢和应激反应的基因被上调,而细胞周期相关基因被下调。小GTP酶Rac1被高度上调,免疫印迹法证实了这一点。我们通过免疫组织化学表明,Rac1在人和小鼠结肠组织隐窝间表的成熟结肠细胞中表达。这些结果支持了先前的发现,即阿司匹林在高浓度和低浓度时具有不同作用,并进一步表明了DNA阵列技术在研究药物作用机制中的应用。此外,它们还指出Rac1在阿司匹林对结肠癌的作用中发挥作用。