[关键词]
[摘要]
核转录因子-κB(NF-κB)控制500个以上基因的表达,是炎症、细胞增殖与凋亡的下游调节中心,其在人类健康的诸多方面(包括先天与后天性免疫的发生与发展)起着重要的作用。NF-κB的降解与许多疾病如癌症、慢性炎症有关。尽管有大量文献报道了源自天然或人工合成的NF-κB抑制剂,然而这些调节子并不能充分地针对治疗目的,因此寻找有医疗用途、副作用小、高效、特异的NF-κB抑制剂仍然是当前研究的重点。来源于植物的天然产物及其衍生物主要有酚类、萜类、生物碱类、木脂素类等物质,近年来有越来越多的新化合物被分离与鉴定,并具有良好的药用价值。开发治疗癌症和免疫失调等与NF-κB相关疾病的有效、安全的药物,植物源天然产物是具有前景的先导化合物来源。针对近年来出现的植物源NF-κB抑制剂进行简要的概述。
[Key word]
[Abstract]
Plant secondary metabolites (natural products) have been a source for many medicines. Their functions in plants often remain unknown, but in recent years there are more and more new compounds isolated and identified and their medicinal potentials are investigated. The major classes of plant natural products and various derivatives thereof are: phenolics, terpenoids, alkaloids, and lignans. The major transcription factor, nuclear factor-κB (NF-κB) is a central downstream regulator of inflammation, cell proliferation, and apoptosis which controls the expression of more than 500 genes. It plays an essential role in several aspects of human health including the development of innate and adaptive immunity. The degradation of NF-κB is associated with many ailments including cancer and chronic inflammatory diseases. In spite of a vast literature describing NF-κB inhibitors from many natural or synthetic sources, such modulators have not been fully tapped for therapeutic purposes and the search for effective and specific inhibitors for therapeutic use with fewer side effects is still relevant and ongoing. Plant-derived phytochemicals are promising the lead compounds to develop potent and safe inhibitors for cancer and inflammatory disorders driven by NF-κB. The recent knowledge on the plant-derived phytochemicals and their major NF-κB molecular targets are briefly reviewed in this paper.
[中图分类号]
[基金项目]
国家自然科学基金资助项目(81360627);江西省自然科学基金资助项目(20132BAB205088)