SMART Institute of Advanced Biomedical Science, Konkuk University, Seoul, Korea.
Mol Nutr Food Res. 2012 May;56(5):761-74. doi: 10.1002/mnfr.201100651.
Natural flavanones exhibit cancer preventive and/or therapeutic effects. The objective of this study was to investigate the molecular mechanism underlying the action of the antitumor activity of hydroxyflavanone using the HCT116 colon cancer cell line.
We investigated the effect of hydroxyflavanones on antitumor activity. We found that 2'-hydroxyflavanone (2'-HF) potently inhibited the clonogenicity of HCT116 cells. 2'-HF triggered apoptosis in both wild-type and p53-null HCT116 cells, as revealed by DNA fragmentation and caspase activation. 2'-HF upregulated nonsteroidal anti-inflammatory drug-activated gene 1 (NAG-1) expression through induction of Egr-1. Silencing of NAG-1 or Egr-1 using small interfering RNA (siRNA) could attenuate 2'-HF-induced apoptosis. Egr-1 also upregulated the proapoptotic gene Bax and the cell cycle inhibitor p21.
Dietary 2'-HF may possess antitumor activity against human colon cancer.
天然类黄酮具有预防和/或治疗癌症的作用。本研究的目的是使用 HCT116 结肠癌细胞系研究羟基黄烷酮抗肿瘤活性的作用机制。
我们研究了羟基黄烷酮对肿瘤抑制活性的影响。我们发现 2'-羟基黄烷酮（2'-HF）能强烈抑制 HCT116 细胞的集落形成能力。2'-HF 通过诱导 Egr-1 使野生型和 p53 缺失的 HCT116 细胞发生细胞凋亡，表现为 DNA 片段化和半胱天冬酶激活。2'-HF 通过诱导 Egr-1 上调非甾体抗炎药激活基因 1（NAG-1）的表达。使用小干扰 RNA（siRNA）沉默 NAG-1 或 Egr-1 可减弱 2'-HF 诱导的细胞凋亡。Egr-1 还上调了促凋亡基因 Bax 和细胞周期抑制剂 p21。
饮食中的 2'-HF 可能具有抗人类结肠癌的抗肿瘤活性。
