Das Joydip, Ramani Rashmi, Suraju M Olufemi
Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States.
Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, United States.
Biochim Biophys Acta. 2016 Oct;1860(10):2107-21. doi: 10.1016/j.bbagen.2016.06.022. Epub 2016 Jun 29.
Naturally occurring polyphenols found in food sources provide huge health benefits. Several polyphenolic compounds are implicated in the prevention of disease states, such as cancer. One of the mechanisms by which polyphenols exert their biological actions is by interfering in the protein kinase C (PKC) signaling pathways. PKC belongs to a superfamily of serine-threonine kinase and are primarily involved in phosphorylation of target proteins controlling activation and inhibition of many cellular processes directly or indirectly.
Despite the availability of substantial literature data on polyphenols' regulation of PKC, no comprehensive review article is currently available on this subject. This article reviews PKC-polyphenol interactions and its relevance to various disease states. In particular, salient features of polyphenols, PKC, interactions of naturally occurring polyphenols with PKC, and future perspective of research on this subject are discussed.
Some polyphenols exert their antioxidant properties by regulating the transcription of the antioxidant enzyme genes through PKC signaling. Regulation of PKC by polyphenols is isoform dependent. The activation or inhibition of PKC by polyphenols has been found to be dependent on the presence of membrane, Ca(2+) ion, cofactors, cell and tissue types etc. Two polyphenols, curcumin and resveratrol are in clinical trials for the treatment of colon cancer.
The fact that 74% of the cancer drugs are derived from natural sources, naturally occurring polyphenols or its simple analogs with improved bioavailability may have the potential to be cancer drugs in the future.
食物来源中天然存在的多酚对健康有巨大益处。几种多酚类化合物与疾病状态的预防有关，如癌症。多酚发挥其生物学作用的机制之一是干扰蛋白激酶C（PKC）信号通路。PKC属于丝氨酸 - 苏氨酸激酶超家族，主要参与靶蛋白的磷酸化，直接或间接控制许多细胞过程的激活和抑制。
尽管有大量关于多酚对PKC调节的文献数据，但目前尚无关于该主题的全面综述文章。本文综述了PKC - 多酚相互作用及其与各种疾病状态的相关性。特别讨论了多酚、PKC的显著特征，天然存在的多酚与PKC的相互作用以及该主题的未来研究前景。
一些多酚通过PKC信号通路调节抗氧化酶基因的转录来发挥其抗氧化特性。多酚对PKC的调节是同工型依赖性的。已发现多酚对PKC的激活或抑制取决于膜、Ca(2+)离子、辅因子、细胞和组织类型等的存在。两种多酚，姜黄素和白藜芦醇正在进行治疗结肠癌 的临床试验。
74%的抗癌药物来自天然来源，天然存在的多酚或其具有改善生物利用度的简单类似物未来可能有潜力成为抗癌药物。
