Division Experimental Tumorpathology, Institute for Pathology, University Erlangen-Nuremberg, Erlangen, Germany.
Front Biosci (Landmark Ed). 2012 Jan 1;17(1):129-73. doi: 10.2741/3919.
Epigenetic mechanisms are essential for normal development and maintenance of adult life. Disruption of epigenetic processes results in deregulated gene expression and leads to life-threatening diseases, in particular, cancer. Global epigenetic alterations are a hallmark of cancer. Cancer epigenetics revealed the deregulation of all components of the epigenetic machinery including DNA methylation, histone modifications, chromatin structure, and non-coding RNAs. Drugs targeting epigenetic processes, or "epi-drugs", are at the forefront of drug discovery, and plant-derived compounds have shown promise. Most of the plant-derived anticancer drugs that work through epigenetic mechanisms are polyphenols; the others are alkaloids, organosulfur compounds, and terpenoids. This review focuses on the epigenetic machinery and its basis for cancer therapy, highlights plant-derived anticancer drugs with epigenetic mechanisms of action, and discusses their potential use in epigenetic therapy.
表观遗传机制对于正常的发育和成人生活的维持至关重要。表观遗传过程的破坏会导致基因表达失调,从而导致危及生命的疾病,特别是癌症。全球表观遗传改变是癌症的一个标志。癌症表观遗传学揭示了包括 DNA 甲基化、组蛋白修饰、染色质结构和非编码 RNA 在内的表观遗传机制的所有成分的失调。针对表观遗传过程的药物,或“表观遗传药物”,处于药物发现的前沿,植物来源的化合物显示出了希望。通过表观遗传机制起作用的大多数植物来源的抗癌药物是多酚;其他的是生物碱、有机硫化合物和萜类化合物。这篇综述重点介绍了表观遗传机制及其作为癌症治疗的基础,强调了具有表观遗传作用机制的植物来源的抗癌药物,并讨论了它们在表观遗传治疗中的潜在用途。